Anti-Cholesterol Drugs Flashcards
1
Q
What are the classes of anti-cholesterol drugs?
A
- Statins
- Fibrates
- PCSK9 inhibitors
- siRNA of PCSK9
2
Q
What is the mechanism of action of statins?
A
- Statins block HMG CoA reductase
- Statins competitively block the active site of the first and key rate-limiting enzyme in the mevalonate pathway, HMG-CoA reductase
- Inhibition of this site prevents substrate access
- This prevents conversion of HMG-CoA to mevalonic acid (which is the precursor to cholesterol)
3
Q
What conditions are statins used for?
A
- Hypercholesterolaemia
- Diabetes
- Angina
- Myocardial infarction
- Cerebral vascular accident
- Transient ischaemic attack
- High risk of MI and CVA
4
Q
What are some side effects of statins?
A
- Myopathy
- Rhabdomyolysis, renal failure
5
Q
What are some examples of statins?
A
- Simvastatin
- Atorvastatin
6
Q
What is the mechanism of action of fibrates?
A
- Fibrates act by decreasing serum triglycerides
?
7
Q
What conditions are fibrates used for?
A
- Hypertriglyceridaemia
- Low HDL cholesterol
8
Q
What is an example of a fibrate?
A
Bezafibrate
9
Q
What is the mechanism of action of PCSK9 inhibitors?
A
- PCSK9 binding promotes LDL receptor degradation within the liver (this is bad)
- PCKS9 inhibitors work by inhibiting the binding of PCSK9 to LDL receptors
- This increases the number of LDL receptors available to clear LDL
- This lowers LDL cholesterol levels
- PCSK9 inhibitors are monoclonal antibodies
10
Q
What condition is a PCSK9 inhibitor used for?
A
Familial hypercholesterolaemia
11
Q
What are examples of PCSK9 inhibitors?
A
- Alirocumab
- Evolocumab
12
Q
What is the mechanism of action of Inclisiran?
A
- Inclisiran is a small interfering RNA (siRNA) that limits production of PCSK9
- It turns off the gene PCSK9
- This boosts the liver’s ability to remove harmful cholesterol from the blood
13
Q
What conditions is Inclisiran used for?
A
- Primary hypercholesterolaemia
- Mixed dyslipidaemia
