Therapeutic Considerations Flashcards
What are the drugs of choice for lowering LDL?
-statins
Which status are the most potent? Least potent?
- most potent = atrovastatin and rosuvastatin
- least potent = fluvastatin
Which statins are metabolized by P450 3A4?
-lovastatin, simvastatin, and atorvastatin
What do the inhibitors of P450 3A4 increase the risk of?
-myopathy
Which statins are metabolized by a cytochrome P450 mediated pathway? (not P450 34A)
-fluvastatin and pitvastatin
Which statins are not metabolized by cytochrome P450s? When should these drugs be considered?
- prvastatin and rosuvastatin
- they should be chosen for patients who are currently taking drugs that are metabolized by cytochrome P450s
Which drugs can be used with statins to further lower LDL levels?
-bile acid sequestrants or cholesterol absorption inhibitors
Which drug can be used with statins for treatment of high LDL and low HDL? What is a risk?
- niacin
- risk of myopathy when taken together
Which drug decreases statin clearance and raises plasma concentration of statins? What is the risk?
- gemfibrozil
- risk of rhabdomyolysis
What are the therapeutic effect of the inhibitors of bile acid absorption?
- lower LDL levels dose-dependently, increase HDL modestly
- also raise triglycerides (undesirable effect)
What are the second-line agents for lipid reduction?
-inhibitors of bile acid absorption
When are inhibitors of bile acid absorption used of statins?
-hyperlipidemia in young patients and in patients for whom statins alone do not provide sufficient LDL reduction
What side effects limit patient adherence to treatment with inhibitors of bile acid absorption?
-significant bloating and dyspepsia
Which class of drugs decreases the absorption of fat soluble drugs? What are the side effects?
- inhibitors of bile acid absorption
- bleeding may result due to vitamin K deficiency; bind certain drugs such as digoxin and warfarin
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?
- 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
Where is ezetimibe absorbed?
-it is absorbed by enterocytes and circulates enterohepatically
Which drugs cause an increase in ezetimibe levels?
-cyclosporine and fibrates
Ezetimibe can increase the plasma concentration of which drug?
-cyclosporine
Which class of drugs are the drugs of choice for hypertriglyceridemia?
-fibrates
What is an important risk of combining fib rates with statins?
-increased risk of myopathy
Does fenofibrate or gemfibrozil have fewer GI and myopathy adverse effects?
-fenofibrate
Fibrates increase the levels of which other drug?
-warfarin
Which side effect of niacin limits its use? How can it be prevented?
-flushing occurs during the first few weeks of use and can be prevented by pretreatment with aspirin
What are two major side effects of niacin, other than flushing?
- hyperuricemia my precipitate gout
- it is associated with impaired insulin sensitivity
What is the prescription strength omega-3 fatty acid?
-Lovaza
