Cardio-Vascular. Anti-lipidemics Statins, Fibrates, Niacin, Omega3, ezetimide… 8/2010 NUR 7755. HYPERLIPIDEMICS. Fats…not water soluble…. Total Chol Trigs. LIPOPROTEINS HDL LDL IDL VLDL Chylo-microns. PEOPLE don’t clog interstate… Chol. and Trigs don’t clog arteries….
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Statins, Fibrates, Niacin,
Fats…not water soluble….
PEOPLE don’t clog interstate…
Chol. and Trigs don’t clog arteries…
cell membranes formation
needed for ADEK vit absorption
Stored in gb as bile
Requires transport protein
Replete w/ dietary trigs ->deliver trigs to skeletal muscle and adipose tissue
apo B 48 (SI)
Source: dietary fat
Catabolized by lipoprotein lipase ->
to Chylomicron remnants ->
return to liver
Free cholesterol liberated
Trigs converted to FFA
Synth. in liver
Lots of Chol
..not counted cholesterol..
VLDLFredrickson-Levy-Lees Classification of Hyperlipoproteinemia
CYP2C19: plavix response
’s coag. ->CVD risk x3.
Homocysteine by-product of methionine
Response to lipid rx
“National Cholesterol Education Program (NCEP)
Adult Treatment Panel III (ATP III)”
Risk stratification and treatment guidelines
Framingham risk stratification
NO risk factors<160
1-2 RF <130
High risk <100
MOA: inhibits enzyme HMG-CoA reductase
Thus: cholesterol synthesis
Thus: synthesis of LDL receptors
Thus: LDL clearance
Dosage 10mg 20mg 40mg 80mg
1998: FDA banned Cholestin
2001: decision reversed on appeal; FDA sent Warning Letters to companies selling red yeast rice; disappeared x yrs
2003: began to reappear
2007: FDA :consumers should not buy or eat red yeast rice products, may contain an unauthorized harmful drug
2010: 30+ brands available. Many avoid FDA restriction by not having any appreciable moncolin content.
Labels / websites say no more than "fermented according to traditional Asian methods" or "similar to that used in culinary applications.” (no mention of cholesterol)
If they do not contain/claim to contain lovastatin, and do not make a claim to cholesterol-> not subject to FDA action.
monacolin content of red yeast rice dietary supplements can vary widely.
Activates “Peroxisome Proliferator Activated Receptor type alpha”(PPARα).
Activate peroxisome proliferator activated receptor a (PPAR a)
Absorbed in intestine
hydrolyzed by esterases in intestine to form active metabolite fenofibric acid
then hepatic glucuronidation
T 1/2 fenofibric acid 20hr (134-200 qd)
60%excreted in urine
25% in feces
May involve reduction or hydrolysis of drug
Phase 2: involves conjugation -
Gemfibrozil inhibits glucuronidation and cyp450 metab of statins
“Changes in CYP enzyme activity may affect the metabolism and clearance of various drugs.
if one drug inhibits the CYP-mediated metabolism of another drug, the second drug may accumulate within the body to toxic levels.”
Thus ’sAUC & Cmax of all statins (except fluvastatin)
Blocks breakdown of fats in adipose tissue
Make sure it’s nicotinic acid!!
n−6:n−3 fatty acids in oils:
cottonseed (almost no n−3)
peanut (no n−3)
grapeseed oil (almost no n−3)
corn oil 46:1
SE: fish burp (freeze)
-made in liver
-stored in gb
-released in to duodenum
Where it emulsifies fats:
-hydrophilic & hydrophobic side, thus aggregate around fat (trigs & phospholipids)
to form micelles
Then absorbed by intestinal villi
Cl- ions for bile
->excrete in feces
6 tab qd; w/meals; other drugs >4hr pre
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