Treatment of Hypercholesterolaemia

Question 1

How do Statins work?

Answer 1

They inhibit HMGCR
- Leads to a decrease in de novo cholesterol synthesis

Upregulate LDL receptors in the liver
- Decreased levels of circulating LDLs

Decrease in expression of adhesion molecules and chemokine receptors

Question 2

How do Fibrates work?

Answer 2

e.g. bezafibrate, ciprofibrate

gene regulatory PPAR agonists

• Increase synthesis of LPL
• > Increased hydrolysis of triglycerides

Question 3

How do Bile Acid Resins (Anion exchange resins) work?

Answer 3

e.g. Cholestyramine

Bind bile acids in the gut and prevent enterohepatic circulation of bile acids
- decreased absorption of exogenous cholesterol

Increased synthesis of bile acids from endogenous cholesterol
- decrease in endogenous cholesterol

Increased expression of LDL receptors

Question 4

Bile Acid Resins have to be used in combination with…

Answer 4

A reduced cholesterol diet

Question 5

What is the role of ADP?

Answer 5

Activates the platelet plug via positive feedback

- May be a target for antithrombotic agents

Question 6

How does Clopidogrel work?

Answer 6

Pro-drug

Inhibits ADP induced platelet aggregation by blocking P2Y12 receptors

Question 7

What is Glybera?

Answer 7

It targets LPL

it is an adeno-associated viral vector that encodes LPL
- treats LPL deficiency!