Drugs that Lower Cholesterol and Triglyceride Levels

Component of all cell membranes and is required for synthesis of:
-Hormones
-Bile salts

Exogenous: dietary sources
Endogenous:
-manufactured in the body, primarily the liver
-An enzyme,(HMG CoA), is an essential catalyst in the hepatic synthesis of endogenous cholesterol

-Serve as carriers for transporting cholesterol and triglycerides in the blood b/c they allow them to become soluble for transport
-LDL & HDL lipoproteins are primarily composed of cholesterol

-Higher percentage of protein and less lipid
-Promote cholesterol REMOVAL (carrying it back to liver for storage)

-Lower percentage of protein
-DELIVER cholesterol to the tissues
-Contribute significantly to heart disease and primary targets of drug therapy

(very low density) lipoproteins contain triglycerides as their core lipids

An essentail catalyst in the hepatic synthesis of endogenous cholesterol

-Widely effective, used, and minimal SEs
-Inhibit HMG CoA reductase decreasing cholesterol production and increasing synthesis of LDL receptors on liver cells which removes cholesterol
-Responses are dose dependent occuring w/in 2 weeks; given orally
-Prototype: lipitor

-Statin
-DON'T TAKE WHEN PREGNANT
-Hepatotoxicity RARE- monitor liver function; myositis RARE

-Do not take with macrolides and grapefruit juice

-Cholestyramine and colestipol
-Form an insoluble mass with bile salts in the intestine increasing their excretion
-LDL levels lowered b/c they're used to create new bile acids
-Excreted unchanged in the stool

-Nausea, bloating, constipation
-No systemic absorption

A new drug in this category (resins) that is better tolerated and does not block the absorption of fat soluble vitamins and most drugs

Decreases the production of VLDLs
-Increases HDL levels more effectively than any other drug
-SEs more common

Intense flushing and itching, GI upset, hepatotoxicity

-Most affective drugs for reducing VLDL levels
-Raise HDL levels but do not reduce LDL levels

Ezetimibe: a new drug that acts on the cells of the intestinal brush border to block cholesterol absorption
-Used adjunct to diet modification, often in combination w/ statins
-Generally well tolerated