Lipid lowering drugs Flashcards
Where is the commonest genetic fault in FH?
LDL receptor
What diet plan can help reduce cholesterol?
Portfolio diet and the UCLP (ultimate cholesterol lowering plan)
List the commonest drugs used to lower cholesterol.
- HMG-CoA reductase inhibitors (statins)
- Ezetimibe
- PCSK-9 inhibitors
- Fibrates
- Colesevelam
- Omega -3 fish oil
What enzyme changes HMU-CoA to mevalonate?
HMU-CoA reductase
What do statins do?
Block the HMU - CoA reductase enzyme
List the major adverse effects of statins?
- generally well generated
- muscle pain - more rarely myositis / rhabdomylosis
- GI disturbance (diarrhoea)
- Liver enzyme abnormalities
How does ezetimibe reduce cholesterol?
It blocks the Niemann-Pick C1 protein which reduces absorption of cholesterol across the gut wall
What do PCSK9 inhibitors cause to happen in cells?
The cells continuously recycle LDL receptors, the receptor goes out to the surface and takes LDL in. This is because if the PCSK9 is inhibited, nothing will signal the receptor not to recycle the receptor
What is the problem with PCSK9 inhibitors ?
They are too expensive
How do you administer PCSK9 inhibitors ?
Subcutaneous injection every fortnight / month of the antibody based treatment
How do fibrates work ?
They work in the nucleus and they turn on a transcription factor called PPAR alpha and they turn on lipoprotein lipase
Where do fibrates especially work?
Liver and muscles
What do fibrates do?
Reduces VLDL and triglycerides
Why don’t we use gemfibrozil anymore?
High interaction risk
What does colesevelam do?
It binds to the cholesterol in your gut and stops your body from absorbing it
