They inhibit the enzyme HMG-CoA reductase
This blocks substrate access and prevents the conversion of HMG-CoA to mevalonic acid and therefore reducing LDL cholesterol synthesis.
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What are some side effects and controversies of statin use?
Myalgia
Type II diabetes
Liver damage
Cognitive damage
Controversies that they dont work well for one in two people
Fears of mental health side effects
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What are fibrates used for?
The treatment of severe resistance dylipidemia
Increase lipoprotein lipase and the breakdown of vLDL and chylomicrons
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What is the mechanism of action of PCSK9 inhibitors?
PCSK9 breakdown the LDL receptors meaning we get a build up of LDL cholesterol so if we inhibit PCSK9 more LDLR are present therefore LDL is broken down.
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What are some examples of PCSK9 inhibitors?
evolocumab and arilocumab
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What are some examples of fibrates?
gemfibrozil and bezafibrate
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What drugs inhibit the endogenous pathway of cholesterol?
Statins
Fibrates
PCSK9 inhibitors
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What drugs inhibit the exogenous pathway of cholesterol?
Cholesterol absorption inhibitors?
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What is the mechanism of action of cholesterol absorption inhibitors (ezetimibe)?
Binds to cholesterol transporter in the duodenum (NPC1L1) and prevents the uptake of cholesterol from the diet
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What is the mechanism of cholesterol absorption inhibitors (bile-acid binding resins -colestyramine)?
Isolate bile acids in the intestine as bile acids contain cholesterol
Cholesterol is then removed from the body
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What is dyslipidemia?
An abnormal amount of lipids in the blood
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What are some primary disorders leading to dyslipidemia?
What are some secondary disorders leading to dyslipidemia?
Hyperthyrodism
Type 2 diabetes
Alcohol abuse
Thiazide diuretics
Beta blockers
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What are apolipoproteins?
Small proteins which bind lipids and allow transport
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Where are exogenous sources of lipids absorbed from?
Absorbed from intestines as chylomicrons
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Where are endongenous sources of lipids made and secreted?
Made in the liver and secreted as vLDL.
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Other cards in this set
Card 2
Front
What are some side effects and controversies of statin use?
Back
Myalgia
Type II diabetes
Liver damage
Cognitive damage
Controversies that they dont work well for one in two people
Fears of mental health side effects
Card 3
Front
What are fibrates used for?
Back
Card 4
Front
What is the mechanism of action of PCSK9 inhibitors?
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