ANTI-HYPERLIPIDEMIC DRUGS
HMG-COA INHIBITORS
Lovastatin; Atarvostatin Analogs of HMG (3-hydroxy-3 methylglutaryl-
CoA) HMG-CoA reductase catalyzes synthesis of
mevalonic acid from HMG-CoA and is the rate limiting step in cholesterol biosynthesis
Leads to up-regulation of LDL receptors in liver
ACTIONS Decrease LDL by 20 – 55% Decrease TG by 10 – 35% Slight increase in HDL
HMG-COA INHIBITORS
Adverse Hepatotoxicity (check ALT and AST, if >3x normal...stop
drug) Myopathy (w/ rhabodmyolysis) and may cause
myoglobinuria which may lead to urine obstruction (measure CPK levels) Increased chances when mixed with fibric acid
derivatives (gemfibrizol), niacin, or P450 3A4 inhibitors CATEGORY X in pregnancy
Therapeutic Uses Great for all hyperlipidemias involving increased levels
of LDL or cholesterol Atherosclerosis; stroke prevention Primary prevention of CAD
BILE ACID RESIN
Cholestyramine Anion-exchange resin – binds bile acids in
intestinal lumen preventing enterohepatic circulation (this increases excretion of bile which is made from cholesterol) this causes an up-regulation of hepatic LDL receptors and increased production of cholesterol
Action: decreases LDL by 10 – 35% Not absorbed at all
BILE ACID RESIN
Adverse Constipation, flatulence, dyspepsia Hypertriglyceridemia Hyperchloremic acidosis (since they exchange
Cl) Bind many things (drugs, vitamins, toxins,
anything fat soluble) which limits their absorption
Prexisting coagulopathy is a contraindication since they prevent absorption of vit K
Uses Hyperlipidemias involving ISOLATED
INCREASES OF LDL Diarrhea from excess fecal bile resins
VLDL SECRETION INHIBITORS
NIACIN (vit B3) MoA: inhibition of VLDL production by
hepatocyte decreases TG synthesis in liver; inhibition of Hormone sensitive lipase in adipose; stimulation of LPL which causes hydrolysis of VLDL
Actions Decreases LDL by 15-25% Decreases VLDL by 40% Decreases TG by 30 – 50% Increases HDL by 15-30% (niacin is MOST
EFFECTIVE in increasing HDL levels!!)
VLDL SECRETION INHIBITORS Adverse
Cutaneous flush (prevented with NSAID) Stimulates histamine release pruritis, rash, nausea, etc Decreased glucose tolerance (contra in DM pts) Hyperuricemia (inhibits tubular secretion of uric
acid) Lowers fibrinogen (good for AS; bad for coag
disorders) Hepatotoxicity (check AST, ALT levels) Rhabdomyolysis (especially when given with
Statins) Uses
Hyperlipidemias with very high VLDL and LDL Pts with very low HDL (despite risk factors you should
give niacin)
FIBRIC ACID DERIVATIVES
Gemfibrozil MoA: activation of nuclear transcription
receptor to increase LPL synthesis (removes TGs from lipoproteins); enhanced removal of VLDL from plasma
Actions Decreases TG by 30-60% Decreases VLDL by 30% Increases HDL by 5 – 10%
FIBRIC ACID DERIVATIVES
Adverse Myopathy (rhabdomyolysis) when
combined with statins Cholesterol levels may actually increase Cholethiasis due to increased biliary
excretion of cholesterol Therapeutic Uses
DOC fro type III lipoproteinemia (familial dysbetalipoproteinemia)
Hypertriglyceridemias
INTESTINAL STEROL ABSORPTION INHIBITOR
Ezetimibe Localizes at the brush border, selectively
inhibits intestinal absorption of cholesterol and related sterols (only blocks exogenous sterol intake)
Actions Decreases LDL by 15-20% Decreases TG by 5-8% THIS DRUG IS WEAK ALONE
INTESTINAL STEROL ABSORPTION INHIBITOR
Adverse Hypersensitivity reactions Severe hepatic disease prolongs drug life
Uses Combined with statins for hyperlipidemias
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