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26 Cards in this Set

  • Front
  • Back
what are the 3 sources of cholesterol for the liver?
de novo synthesis
cholesterol absorbed by small intestine
lipoproteins circulating in blood
what is the rate limiting enzyme involved in the synthesis of cholesterol?
HMG CoA reductase
HMG CoA reductase inhibitors
ends in statin
HMG CoA reductase inhibitor prevents the productiong of?
mevalonate and then cholesterol
MOA of HMG CoA reductase inhibitor
upregulate LDL receptor to remove LDL from blood circulation
what effects will statin have on triglycerides?
modest reduction
what effects will statin have on LDL?
large reduction
the greatest LDL lowering effect is seen at the usual starting dose of a statin True or False
True
Pravastatin is metabolized by P450 system true or false
false
which two statin drugs have longer half life?
atorvastatin and rosuvastatin
when is hepatic cholesterol synthesis maximal at day or night?
night, between 12 to 2 am
should statin be taken at night or day?
night (before bed)
HMG CoA reductase inhibitor SE
rhabdomyolysis
Fibrates (especially gemfibrozil)
Niacin (rarely)
CYP3A4 inhibitors
Cyclosporine
Azole antifungals (ketoconazole)
Erythromycin
Grapefruit juice (inhibit gut wall CYP3A4)
drug interaction of HMG CoA reductase inhibitor
contraindications of HMG CoA reductase inhibitor
Active hepatic disease
Pregnancy and lactation
Fetus requires cholesterol to develop cell membranes during growth
bile acid binding resin agents
Cholestyramine (Questran, Locholest, Prevalite)
Colestipol (Colestid)
Colesevelam (Welchol)
MOA of bile acid binding resin
reduce bile recirculation
increase for bile synthesis
upregulate LDL
remove LDL from blood
would you combine statin and bile acid binding resin?
yes
Would cholestyramine be indicated for the treatment of hypertriglyceridemia?
NO
do bile acid binding resin agents come in tablet and powder forms?
Yes
what is the rationale for taking bile acid binding resin before meals?
eating stimulate bile acid synthesis and release
Ezetimibe (Zetia)
cholesterol absorption inhibitor
MOA of ezetimibe?
decrease cholesterol delivery from the intestine to the liver
what does ezetimibe affect the clearance of cholesterol from the blood?
increases
clofibrate, gemfibrozil, fenofibrate
fibric acid derivatives
what effect does fibric acid derivatives have on TG?
large decrease