Anti-Dyslipidemics Flashcards
HMB-CoA reductase Atorvastatin calcium (Lipitor)
HMB-CoA reductase is the rate limiting step key enzyme to producing cholesterol
1st line tx for hypercholesterolemia
2 main effects:
Lower LCL
Increase HDL
ADDED BENEFITS make popular 1st line choice!
CYP450 metabolism
HMB-CoA reductase Atorvastatin calcium (Lipitor)
HMB-CoA reductase is the rate limiting step key enzyme to producing cholesterol
1st line tx for hypercholesterolemia
2 main effects:
Lower LCL
Increase HDL
ADDED BENEFITS make popular 1st line choice!
CYP450 metabolism
Fibric acid derivatives, PPARa activator
Fenofibrate (Tricor)
Agonist at peroxisome proliferator activated receptor (PPAR-a)
Increase fatty acid oxidation
Increased activity of lipoprotein lipases = breakdown TGs
= DECREASE TGs main action
Tx: patients with severe hypertriglyceridemia
*excrete by kidney
Bile Acid binding resins
Colesevelam (welchol)
Bind bile acids in the intestines and prevent their reabsorption
can bind other drugs on accident too not selective
Leads to increase breakdown of hepatic cholesterol because it is not recycled
Main action: decrease LDL (small effect for dyslipidemia = USE IN COMBO)
Nicotinic acid
Niacin
2 actions:
- Adipose tissue - Inhibit lipolysis of TGs by lipase (decrease hepatic synthesis)
- Liver - Reduce TG synthesis by inhibiting synthesis and esterification of FAs
3 beneficial effects:
Lower TG
Lower LDL
Increase HDl
cutaneous flush
Cholesterol absorption inhibitor
Ezetimibe
Inhibits intestinal absorption of cholesterol transport protein (Nieman Pick NPC1)
Reduces LDL
Not better than statin alone
Lose favor because interacts with MANY DRUGS
LDL
Cholesterol
HDL
> 40-60 optimal
Triglycerides
30 less than LDL
Atherogenic proteins
VLDL, LDL, IDL
Anti-atherogenic proteins
HDL
Fibric acid derivatives, PPARa activator
Fenofibrate (Tricor)
Agonist at peroxisome proliferator activated receptor (PPAR-a)
Increase fatty acid oxidation
Increased activity of lipoprotein lipases = breakdown TGs
= DECREASE TGs main action
Tx: patients with severe hypertriglyceridemia
*excrete by kidney
Bile Acid binding resins
Colesevelam (welchol)
Bind bile acids in the intestines and prevent their reabsorption
can bind other drugs on accident too not selective
Leads to increase breakdown of hepatic cholesterol because it is not recycled
Main action: decrease LDL (small effect for dyslipidemia = USE IN COMBO)
Nicotinic acid
Niacin
2 actions:
- Adipose tissue - Inhibit lipolysis of TGs by lipase (decrease hepatic synthesis)
- Liver - Reduce TG synthesis by inhibiting synthesis and esterification of FAs
3 beneficial effects:
Lower TG
Lower LDL
Increase HDl
cutaneous flush
