extra hepatic lipid modifiers Flashcards
Zetia
Ezetimibe, inhibits NPCL1 from transporting cholesterol from the lumen into brush border intestine
Lowers LDL
cholesterol absorption inhibitor
Xenical
Orlistat, inhibits pancreatic lipase inhibiting absorption of dietary fat
fat absorption inhibitor
Zetia ADME
Cholesterol Absorption Inhibitor A: absorbed D:systemic to limited degree 90% protein bound M: glucoronidated E: feces
Orlistat
Fat absorption inhibitor
A: stays in gut, no D, M,
E: feces
Welchol
BETTER TOLERATED
Colesevelam upregs LDLR in liver by binding to - charge bile acid to be excreted in feces (prevent reabsorb cholesterol from bile)
Preferred in Pregnancy
Bile Acid resin
Quetran
Cholestyramine upregs LDLR in liver by binding to - charge bile acid to be excreted in feces (prevent reabsorb cholesterol from bile)
Bile Acid resin
Welchol ADME
Colesevelam no A or M, excreted in feces
can impair absorption fat soluble vitamins
Bile acid Resin
Quetran ADME
Cholestyramine no A or M, excreted in feces
can impair absorption fat soluble vitamins
Bile acid Resin
Niacin
inhibits lipolysis in adipose tissue> prevents liver from using FFA to make VLDL
NOT TOLERATED WELL (flushing, n/v)
MOST EFFECTIVE FOR HDL increase
decrease LDL and TG
Niacin ADME
A- peak plasma 30-60min
D: broad systemic
M: rapid 1st pass
E- mostly urine, some feces
co therapy with statin increased risk myopathy
Lopid
Gemfibrozil increases LPL activity (activates PPARalpha) produce more HDL and LPL can get myositis adverse event DECREASE TG (FIRST LINE PANCREATITIS) fibrate
increased risk with statin MYOPATHY
Tricor
Fenofibrate increases LPL activity (activates PPARalpha) produce more HDL and LPL can get myositis adverse event DECREASE TG (FIRST LINE PANCREATITIS) fibrate increased risk with statin myopathy
Clofibrate
dsctnd, adverse events especially with statin
fibrate
fibrates ADME
A; peak plasma 1-2hrs
D; broad systemic, plasma bound
M; rapid first pass, glucoronidated
E; major glucoronidated urine
Juxtapid
Lopitamide is MTTPI which inhibits transfer of TG to intestinal and liver cells
metabolized by CYP3A4