HLD drugs Flashcards
Rate limiting step of cholesterol synthesis inhibited by statins
HMG-CoA reductase
Result in liver from blocking intrinsic cholesterol synthesis
Upregulation of hepatic LDL receptors resulting in decreased plasma LDL
Therapeutic effect of statins
Decrease in LDL, VLDL, and triglycerides
Mild increase in HDL
Secondary prevention of heart disease by statins
Improve endothelial function
Modulate inflammatory response
Maintain plaque stability
Increase NO and decrease mRNA for endothelin-1 –> vasodilation
Drug interactions of statins
Inhibitors of CyP450 –> grapefruit juice and red yeast rice
Adverse effects of statins
Myopathy
Hepatoxicity
Risk of myopathy in statins increases with what?
Concurrent therapy of gemfibrozil and/or nicotinic acid (niacin/vit B3)
Types of bile acid sequestrants used for HLD
Cholestyramine
Colestipol
Colesevelam
Secondary use of cholestyramine (not HLD)
Used in pruritis due to biliary obstruction
Mechanism of bile acid sequestrans
Bind bile acids in GIT to form insoluble complex that is excreted in the feces
Cholesterol used to make more bile –> results in lowered LDL
Contraindication of bile acid sequestrants
Hypertriglyceridemia –> increases VLDL and triglycerides
Adverse effects of bile acid sequestrants
Fat malabsorption –> steatorrhea
Malabsorption of fat soluble vitamins
Vitamin with lipid lowering effect at high doses
Niacin/nicotinic acid/vit B3
Mechanism of high dose niacin in HLD
Inhibit hepatic production of VLDL and LDL
Decreases HDL clearance
Increases lipoprotein lipase activity
Catalyzes hydrolysis of triacylglycerol component of circulating chylomicrons and VLDL
Lipoprotein lipase