Drugs Used In Hyperlipidemia Flashcards
The longer and lower the reduction in circulating LDL-C, the lower the incidence of
CHD
Cholesterol esters and triglycerides are insoluble in water and circulate in blood as
Lipoprotein particles
Low density lipoprotein ApoB is recognized by the
LDL receptor
The LDL receptor internalizes circulating
LDL
A transcription factor that serves as the master regulator of cholesterol levels in the cell
SREBP (Sterol Regulatory Element Binding Protein)
In a low cholesterol diet, SREBP is
Activated
Results in increase in cholesterol biosynthesis and increase in receptor-mediated LDL endocytosis from the plasma
SREBP activation
In a high-cholesterol diet, SREBP is not activated and thus we see a decrease in
Cholesterol biosynthesis and LDL receptors
The most effective and best tolerated agents for treating dyslipidemia
Statins
Statins function as
HMG-CoA reductase inhibitors
Competitive inhibitors of HMG-CoA reductase
- Inhibits cholesterolgenesis
- Increase expression of LDL receptor
Statins
Inactive lactose pro drugs hydrolysis to active drugs
Statins
Statin absorption varies from 40% to 75% except for
Fluvastatin (almost completely absorbed)
Statins have half-lives of 1-3 hours except for
- ) Atorvastatin?
- ) Rosuvastatin?
- ) 14 hours
2. ) 19 hours
Hepatic cholesterol biosynthesis is maximal from midnight-2 AM, so we want to take them in the
Evening (except for the ones w/ the long half-lives)
Contraindicated in women who are pregnant, lactating, or likely to become pregnant
Statins
Most efficacious agents for severe hypercholesterolemia
-More TG lowering activity compared to other statins
Atorvastatin and Rosuvastatin
Two toxic/adverse effects of Statins are
- ) Hepatotoxicity
2. ) Diabetes Mellitus