2. 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
3. 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
4. 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
5. 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
6. 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!!)
7. 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)
8. 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%
9. 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
10. 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
11. INTESTINAL STEROL ABSORPTION INHIBITOR
Adverse
Hypersensitivity reactions
Severe hepatic disease prolongs drug life
Uses
Combined with statins for hyperlipidemias
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