Hypolipidemic Agents Flashcards
Condition when blood triacylglycerol or cholesterol in lipoproteins exceeds normal?
Hyperlipoproteinemia
Elevated lipoprotein accelerates development of 3 types of atherosclerosis
- Peripheral vascular disease (thrombosis) 2. Ischemic cerebrovascular disease 3. Coronary heart disease (CHD or myocardial infarction)
All of the carbon atoms of Cholesterol are derived from…?
the acetate of Acetyl-CoA
Statins inhibits which enzyme of cholesterol synthesis?
HMG-CoA Reductase
Dietary lipids are packaged into what in the Exogenous Pathway?
Chylomicrons in the intestinal mucosal cells
Fatty acids/cholesterol synthesized in the liver in addition to lipids taken up from blood produce…?
VLDL
VLDL deliver lipids to peripheral tissues and become IDL and …?
LDL
Process of HDL bringing cholesterol and cholesterol esters back to the liver?
Reverse Cholesterol Transport
What category of drugs is the oldest hypolipidemic drugs?
the “Fibrates”
The 1st “fibrate” on the marker?
clofibrate
what “fibrate” drugs are useful for lowering VLDL?
gemfibrozil and fenofibrate
In the mech of action of “fibrates”: what transcription factor is activated to increase fatty acid oxidation and lipoprotein lipase?
PPARa
Currently available fibrates?
fenofibrate, fenofibric acid, gemfibrozil
1st statin?
lovastatin
Progressive muscle side effects of statins?
myalgia, myopathy and rhabdomyolysis
Baycol problem?
more aggressive statin therapy = greater side effects
Currently available statins?
Atorvastatin (lipitor) and rosuvastatin (preventative therapy)
Fish oils that reduce plasma TG and decrease VLDL synthesis?
EPA and DHA
FDA approved fish oil?
LOVAZA
Recommended dose of Lovaza?
4 grams/day
Fish oils do not lower…?
cholesterol
Hypolipidemic dose of Niacin is…?
about 3 grams
Which B vitamin decreases TAG and increases HDL?
Niacin
Mechanism of action of Niacin is to inhibit…?
hormone sensitive lipase
Niacin preparations available in US?
Polygel extended release niacin and prescription extended release niacin
Mechanism of action of Bile Acid Sequestrants is to…?
block enterohepatic cycling
Which class of hypolipidemic agents greatly decreases absorption of negatively charged drugs?
bile acid sequestrants
Currently available bile acid sequestrants?
cholestyramine, cholestipol, and cholesevalam
Newest class of lipid-lowering agents?
cholesterol absorption inhibitors
Mechanism of action of cholesterol absorption inhibitors: inhibits the … w/o affecting FA uptake?
intestinal cholesterol transporter
Example of cholesterol absorption inhibitor?
ezetimbe
