Lipid Regulating Drugs Flashcards
What is the first line of treatment in hyperlipidaemia?
- lifestyle interventions
As there are no surgeries available for hyperlipidaemia what are the 2 treatment options available?
- lifestyle interventions
- medications
What is 3-hydroxy-3-methyl-glutaryl-coenzyme A (HMG-CoA) reductase?
- enzyme that reduces 3-hydroxy-3-methyl-glutaryl-coenzyme A into mevalonate in cholesterol metabolism
Where is 3-hydroxy-3-methyl-glutaryl-coenzyme A (HMG-CoA) reductase active in the body?
- liver
Why is 3-hydroxy-3-methyl-glutaryl-coenzyme A (HMG-CoA) reductase so important?
- rate limiting step in cholesterol synthesis
- no HMG-CoA) reductase = no mevalonate and no cholesterol
What enzyme is the target for hyperlipidaemia medications?
- 3-hydroxy-3-methyl-glutaryl-coenzyme A (HMG-CoA) reductase
What are the first line of drugs for anyone with hyperlipidaemia?
- statins
What are the 2 statins that we need to know?
- Atorvastatin (most commonly prescribed)
- Simvastatin (dirty drug)
What do statins do to a patients lipid profile?
- ⬇️ cholesterol production by liver
- ⬇️ LDL
- ⬇️ total cholesterol
- ⬇️ triglycerides
- ⬆️ HDL
In addition to treating hyperlipidaemia, what else are statins effective for when considering the development of atherosclerosis plaques?
- -anti-inflammation
- cholesterol in plaques
Statins are able to reduce all cause mortality, what does this mean?
- reduce death from any cause in patients with arterial disease
What are the most common side effect of statins?
- myalgia (most common symptom)
- rhabdomyolysis
- arthralgia (joint pain)
- liver dysfunction
What does rhabdomyolysis mean?
- rhabdo = rod like
- myo = muscle
- lysis = breakdown
Prior to statins being developed, what was the main drug of choice to treat hyperlipidaemia
- fibrates
What is the mechanism of action for fibrates?
Fibrates lower hepatic apoC-III production and increase lipoprotein lipase—mediated lipolysis via PPAR.
Fibrates act on peroxisome proliferator-activated receptor (PPAR)-alpha, what is this?
- a ligand-activated transcriptional factor
- upregulation of fatty acid beta-oxidation (produce energy)
What is the main fibrate we need to be aware of?
- Bezafibrate
What are fibrates, specifically Bezafibrate able to do to the lipid profile?
- ⬇️ LDL
- ⬇️ TAG (main effect)
- ⬆️ HDL
What are side effects of fibrates, specifically Bezafibrate?
- GI disturbance (diarrhoea)
- myalgia (muscle pain)
- rhabdomyolysis
In addition to statins and fibrates there are bile salt sequestrants. How do these drugs affect cholesterol levels?
- bind to bile acids and stops re-absorption - liver has to use cholesterol to make more bile acids - ⬇️ cholesterol
What is the name of the bile salt sequestrants that we need to be aware of?
- Cholestyramine
What is the main side effect of Cholestyramine, a bile salt sequestrants?
- GI disturbance (diarrhoea)
- ⬇️ fat soluble vitamines (A.D.E.K)
Instead of using Cholestyramine, what is a more commonly used bile salt sequestrants?
- Ezetimibe
What is proprotein convertase subtilisin/kexin type 9, more commonly referred to as PCSK9?
- an enzyme involved in cholesterol regulation
- regulates the number of LDL receptors
What do PCSK9 inhibitors do?
- ⬆️ number of LDL receptors
- cholesterol
