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LIPID TRANSPORT Transported as lipo proteins Central core-TG and CE Outer coat-Phospholipid, FC, Apolipoproteins 6 Classes of lipoproteins: chylomicrons, rem, VLDL, LDL ,IDL, HDL
CLASSIFICATION HMG-CoA reductase inhibitors:statins Bile acid sequestrants: resins Fibric acid derivatives:clofibrate Nicotinic acid: Others:probucol
STATINS Lovastatin,simvastatin,atorvastatin,rosuva
M.O.A:inhibits cholesterol synthesis ACTIONS:1.increase in LDL receptor
2. Decrease in LDL, IDL 3. Increase in HDL Statins differ in potency and max efficacy Dose dependent effect Max effect at mid night
ADR:headache,GI upset,rashes,sleep dis,
Increase in liver enzymes Muscle damage and increase in CPK
DI:CYP 3A4 dependent CI:pregnancy,lactation,trauma, illness, surgery8 USES: Primary and secondary hyperlipidemias
IHD: decrease in MI risk and mortality
OTHER EFFECTS: increased CA compliance
plaquestabilization,endothelialfunction, ReducedLDL oxidation, anti inflammatory action BILE ACID SEQUESTRANTS Cholestyramine,colestipol,colesevelam
M.O.A:large polymeric cationic exchange resins which bind bile acids and
prevent their absorbtion
ACTIONS:Cholesterol to bile acids
Clearence of LDL,IDL, LDL receptor up regulation
USES: primary hypercholesterolemia
used in combination pruritus digitalis toxicity
ADR:constipation, bloating ,diarrhea
gallstones,dry skin
DI: Interferes with absorption
FIBRIC ACID DERIVATIVES Gemfibrozil,fenofibrate
M.O.A:Activate lipoprotein lipase Actions:peroxisome proliferator activated receptor alpha(PPARα)
enhances LPL synthesis fattyacid oxidation LDL receptor expression
decrease hepatic TG synthesis degradation of VLDL and circulating TG increase in HDL,decrease in VLDL secretion dysbetalipoproteinemias
USES:Hypertriglyceridemia
ADR:GI symptoms,rashes,myopathy, arrythmias ,hypokalemia ,increase in liver
enzymes NIACIN Nicotinic acid
MOA : inhibits TG synthesis in liver
Inhibits lipolysis in adipose tissue Increases activityof LPlipase
ACTIONS :Decrease in VLDL ,IDL,LDL
Increase in HDL Increase in Tpa Decrease in fibrinogen
USES: wide spectrum hypolipidemic
Adjunctive to statins and fibrates
ADR: Cutaneous vasodilator
GI upset dryness and pigmentation liver dysfunction,hyperglycemia hyperuricemia
DI: postural hypotension, myopathy
NEWER DRUGS
INHIBITORS OF INTESTINAL STEROL ABSORPTION: ezetimibe
MTP INHIBITORS ACAT INHIBITORS
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