Flashcards in 3 - Cholesterol Deck (27):
What are the oxidative effects of LDLs?
Inhibits macrophage activity
Induce T cell activity
Toxic to endothelial cells
Enhance platelet aggregation
Give an example of a statin
Describe the effect of statins
Inhibit cholesterol synthesis in hepatocytes
Increase clearance of LDLs
Decrease production of LDLs
What are the secondary benefits of statins?
Increased endothelial function
Decreased thrombotic risk
What is the mechanism of action of statins?
Deceased serum LDLs and increased synthesis of LDL receptors, so more is taken up by receptors
What are the adverse effects of taking statins?
Increased transaminase levels -indicative of liver damage
Myopathy, potentially developing into rhabdomyalisis
Name an example of a fibric acid derivative
What type of molecule is a fibric acid derivative?
An ampipathic (hydrophobic and phillic) carboxylic acid
What is the mechanism of action for fibric acid derivates?
PPAR alpha agonist, increasing the production of lipoprotein lipase therefore decreasing triglyceride production
What are the effects of taking fibric acid derivatives?
Decreased triglyceride production
Increased fatty acid uptake and oxidation
Increased LDL particle size
What are the side effects of fibric acid derivatives?
Abnormal liver function tests
Myositis (inflamed muscles)
What are the contraindications for fibric acid derivatives?
Gall bladder disease
What are the effects of nicotinic acid?
Decreased lipoprotein synthesis
Therefore reducing coronary events
What are the contraindications for nicotinic acid?
Peptic ulcer disease
Active liver disease or abnormal liver function tests
What are the side effects of nicotinic acid?
Activation of peptic ulcer
Decreased insulin sensitivity
What is the mechanism of action of Ezetimibe?
Selectively inhibits intestinal cholesterol absorption, so less intestinal delivery of cholesterol to liver
What are the effects of Ezetimibe?
Decreased intestinal delivery of cholesterol to liver
Increased expression of hepatic LDL receptors
Decreased cholesterol content of atherogenic particles
What are the side effects of Ezetimibe?
Why is Ezetimibe generally well tolerated?
Circulates enterohepatically, delivering agent back to target site and limiting systemic exposure, producing fewer side effects
What target should be set for cholesterol levels?
2 mmol for LDL
What can statins be given in combination with?
Fibric acid derivatives
What is the danger of giving fibric acid derivatives in combination with statins?
Increased risk of myopathy and rhabdomyolysis
Describe the mechanism of action of PCSK9 inhibitors
Inhibits PCSK9 from internalising LDL receptors, so more receptors are present so can remove more from the bloodstream
What type of molecule is a PCSK9 inhibitor?
A monoclonal antibody
Give an example of a PCSK9 inhibitor
Which dietary factors have a positive effect of cholesterol levels?
Vitamin C and E