Antihyperlipidemic Drugs II Flashcards
what is the cholesterol absorption inhibitor
ezetimbe
mechanism of ezetimbe
- selective inhibitor of a transport protein (NPC1L1) in jejunal enterocytes which takes up cholesterol from lumen –> compensatory increase in cholesterol synthesis (inhibit with statin) –> reduced intestinal cholesterol delivered to liver –> upregulation of LDL receptors –> increased LDL clearance from plasma
really effective as a dual therapy with statin
why is ezetimbe effective even in absence of dietary cholesterol
inhibits reabsorption of cholesterol excreted in bile
what is ezetimbe used for
- as a dual therapy for patients on statin who can’t reach their LDL goal
- only used as monotherapy in those who can’t tolerate statin (more effective as a dual therapy)
adverse effects of ezetimbe
reversible impaired hepatic function
myositis (inflammation and degeneration of muscle tissue)
drug interaction of ezetimbe
bile acid sequestrant (cholestyramine, colestipol, colesevelam) inhibits absorption of ezetimbe so should not be given together
what are the omega 3 FA
EPA, DHA, and Lovaza
what do the fish oils do
EPA and DHA reduce TAG synthesis, increase FA oxidation in the liver, and long term may increase HDL
what does lovaza do
with adjuvant to proper diet can reduce TAGs in pts with high levels ( greater than 500mg/dL)
suggest drug if isolated severe hypertriglyceridemia
fibrate (or niacin or fish oil)
then add a statin
Statin is first line drug for what profiles
elevated LDL
elevated LDL and TAGs
isolated low HDL
which antihyperlipidemic drug is contraindicated in pregnant women
statins
category X
antihyperlipidemic that is teratogenic in animals and should only be used in pregnant women if benefits outweigh the risks
fibrates - gemfibrozil and fenofibrate
category C
antihyperlipidemic drugs that interferes with absorption of nutrients
cholestyramine and colestipol
category C
antihyperlipdemic drug that causes skeletal defects in animals
ezetimbe
category C
