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Antihyperlipidemic Drugs
PHAR450
4
Pharmacology
Undergraduate 4
04/01/2014

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Term
Statins
Definition
Drugs to treat hyperlipoproteinemia
Inhibitors of HMG-CoA reductase, the rate-limiting step in cholesterol synthesis
Useful as secondary preventative treatment in those with pre-existing CVD or risk of heart disease
Also improve endothelial function, modulate inflammation, maintain plaque stability & prevent thrombus formation
Term
Cholestyramine (Questran)
Colesvelam (Cholestagel, Welchol)
Colestipol (Colestid)
Definition
Synthetic polymeric resins used as bile acid sequestrants to treat hyperlipoproteinemia
Resins bind bile acids in the intestine & prevents reabsorption
Decreased bile acid levels induces conversion of cholesterol to bile
Decreases VLDL and LDL, increases HDL
Side effects include severe constipation
Term
Bezafibrate (Bezalip)
Ciprofibrate (Modalim)
Gemfibrozil (Lopid)
Fenofibrate (TriCor)
Definition
Fibric acid derivatives
Drugs to treat hyperlipoproteinemia
Activate PPARs, transcription factors that modulate carb and fat metabolism and adipose tissue differentiation
Term
Niasin (vitamin B3)/nicotinic acid
Definition
Drug to treat hyperlipoproteinemia
Binds a GPCR which causes inhibition of fat breakdown
Reduces the production of triglycerides, VLDL and LDL
Increases HLDL more than other drugs
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