Drugs to prevent atherosclerosis Flashcards
Give examples of statins used to prevent atherosclerosis
Lovastatin
Atorvastatin
What is the mechanism of action of statins
They inhibit 3-hydroxy-3-methyl-glutaryl-CoA reductase, a rate controlling enzyme of the mevalonate pathway which produces cholesterol
what is the function of statins
They decrease liver cholestrol synthesis
They increase the VLDL and LDL receptor expression, and decrease the amount of LDL in the blood
what are the side effects of statins
Myalgias (muscle pain)
Muscle cramps
Rhabdomyolysis (damaged skeletal tissue breaks down rapidly leading to kidney failure)
GI disturbancdes
Malabsorption of lipid soluble vitamins (A, D, E, K) and lipid soluble drugs
Give examples of fibrates used to prevent atherelosclerosis
Bezafibrate
Ciprofibrate
What are fibrates
amphipathic carboxylic acids
what is the mechanism of action of fibrates
agonists of the peroxisome proliferator-activated receptor alpha (PPAR-alpha) receptor
what is the function of fibrates
Increased beta-oxidation in the liver
Decreased hepatic triglyceride secretion
Increased lipoprotein lipase activity causing increased VLDL clearance
Increased HDL
When are fibrates mainly used
Hypercholesterolemia
What are the side effects of the fibrates
Mild stomach upset
Myopathy (muscle pain with creatinine phosphokinase elevation)
Increased risk of gallstones due to increased cholesterol in bile
Increased risk of rhabdomyolysis - especially if added to statins
Give examples of bile acid binding agents used to prevent atherosclerosis
Cholestipol
Cholestyramine
What is the mechanism of action of bile acid binding agents
Bile acid is recycled between the intestine and the liver
Cholestipol and cholestyramine bind to bile acid in the gut leading to an increased loss
What is the function of bile acid binding agents
Decreased enterohepatic recirculation of bile salts
Increased synthesis of new bile salts by the liver
Decreased liver cholesterol
Increased LDL receptor expression, and decrease the amount of LDL in the blood
What are the side effects of the bile acid binding agents
Increases in VLDL and triacyglyceride synthesis
GI tract disturbances
Malabsorption of lipid soluble vitamins (A, D, E, K) and lipid soluble drugs
