LIPID REGULATING DRUGS Flashcards
Treatment aims to: 1. Reduce LDL (bad) cholesterol 2. Increase HDL (good) cholesterol 3. Decrease TG (cardiovascular benefit)
1
Q
HMGCoA reductase inhibitor & MOA
A
STATINS!
-Atorvastatin, Simvastatin, Rosuvastatin, Pravastatin, Fluvastatin
MOA
- INHIBIT the RATE LIMITING ENZYME in the production of endogenous cholesterol
- As a COMPETITIVE INHIBITORS of HMGCoA
2
Q
Effect of STATINS!
A
- Decreased cholesterol production by liver.
- Increased removal of LDL by liver from circulation.
- Reduction of VLDL and TG
- Increased HDL levels (MOA unclear)
3
Q
How is LDL removed by using statins?
A
- Decreased production of endogenous cholesterol
- Increase of LDL receptor production
- Increase of LDL expression
- Increase removal!
4
Q
SIde effects of STATINS!
A
Muscke pain (underreported but relatively common)
Raised liver transaminases/hepatic failure
Fatal hepatotoxicity and myopathy (1 per 1 million)
5
Q
Resins-Bile Acid Sequestrants & MOA
A
RESINS!
-cholestyramine resin
MOA
Binds bile acids in the intestinal lumen and prevent their reabsorption.
6
Q
Effects of RESINS!
A
- Depletes bile acid pool
- Increase synthesis of bile acid –> increase uptake of serum LDL!
- But can increase TG
7
Q
Inhibitors of Cholesterol Absorption & MOA
A
- Plant sterols
MOA: Displace cholesterol from micelles - Ezetimibe
MOA: Selectively inhibits absorption of cholesterol from the intestine/ by blocking the NPC1L1 sterol transport protein.
8
Q
Nicotinic Acid & MOA
A
Niacin
MOA pooly understood:
- in adipose tissue, decrease release of free fatty acids –> less transport to liver
- reduction in hepatic TG synthesis & esterification of free fatty acids
- enhancing LPL activity –> promotes chylomicron and VLDL clearance
