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27 Cards in this Set

  • Front
  • Back

pravastatin ezetimibe

not metabolized by cytochrome p450

fluvastatin, rosuvastatin, pitavastatin

CYP2C9

atorvastatin, simvastatin, lovastatin

CYP3A4

rosuvastatin simvastatin

statins that increase HDL

lovastatin simvastatin

statin prodrugs; penetrate CNS

rosuvastatin

20 hr t1/2, use less in Asians, dec LDL 63% (highest %)

rosuvastatin, avorvastatin

give at any time of day (t1/2 20hr; 14hr)

atorvastatin

decrease LDL 60% (2nd highest), t1/2 14 hr

pitavastatin

t1/2 12 hr

simvastatin

max 40mg (<80mg) -lower dose due to myopathy, lower LDL 51% (3rd best)

lovastatin pravastatin simvastatin

generics

niacin, Gemfibrozil, Fenofibrate, ezetimibe

NOT if gall bladder disease

familial combined hyperlipidemia

overproduce apo-B100 --> inc VLDL and LDL

familial hypertriglyceremia

deficient liporprotein lipase--> inc trig, VLDL

familial hypercholesterolemia

defective LDL-R or defective apo-B100 (LDL not recognized)

niacin mechanism

inhibits hormone sensitive lipase (--> less FFA)


inhibit liver clear. of ApoA-I -->ApoAI--> inc HDL


but inc cholesterol and bile acid secretion

fibric acid derivatce (fenofibrate, gemfibrozil) mechanism

inhibit lipogenesis (liver FA--> trig)


inhibit Apo CIII (so incr. LPL-->inc musc metab)


incr. synth. Apo-AI, AII ---> incr. HDL


incr. size LDL

gemfibrozil

competes with glucaronidation of statins (increased myopathy)

bile acid binding resin mechanism (cholestyramine, colestipol, colesevelam)

bind bile acid - insoluble complex can't be reabsorbed --> decr. chol in liver--> proteases activate SREBP to bind SRE--> incr. LDL-R

cholestyramine colestipol (not colesevelam)

decr. uptake ADEK, warfarin, statins, folic acid;


constipation, bloat, indigestion

statin mechanism

HMG-CoA analog -- inhibit HMG-CoA reductase synthesis of mevalonate

all statin drug-drug interaction

extensive first pass uptake by OATP1B1

ezetimibe (zetia)

selectively inhibit intestinal absorption of cholesterol at brush border small intest. (liver --> glucuronide) --- cholestyramine and colestipol interfere with absorption

mipomersen

inhibit apo-B100 synthesis

limitapide

inhibit MTP

mipomersen limitapide

S/E hepatic steatosis

niacin + resin + statin

lower LDL 70%