Flashcards in Session 3 - Cholesterol Lowering Drugs Deck (17)
What are the main drug groups used to lower LDL cholesterol?
Fibric acid derivatives (fibrates)
What is the mode of action of statins?
Lowers cholesterol synthesis by inhibiting HMG-CoA reductase in the liver. This decreases production of VLDL and LDL as well as increasing clearance of IDL and LDL.
What are the clinical benefits of statins?
Primary benefit: lowers cholesterol
Secondary benefits: anti-inflammatory, plaque reduction, improved endothelial cell function, reduced thrombotic risk.
What adverse drug reactions can statins produce?
Increase transaminase levels
Myopathy (diffuse muscle pain, most commonly seen when statins are combined with another drug such as cyclosporine, gemfibrozil)
Gives three examples of statins.
What is the mode of action of fibrates?
Increases fatty acid uptake and oxidation
Reduces triglyceride levels
Direct vascular effects
What adverse drug reactions can fibric acid derivatives produce?
What are the contraindications for using fibric acid derivatives?
Hepatic or renal dysfunction
Pre-existing gallbladder disease
Give some examples of fibric acid derivatives.
PPAR alpha (peroxisome proliferator activated receptor) agonist
What is the mechanism of action of Peroxisome Proliferator Activated Receptor (PPAR alpha) agonists?
Increase the production of lipoprotein lipase
What is the mode of action of nicotinic acid?
Lipid lowering effect by inhibition of lipoprotein synthesis. Reduces VLDL and increases HDL at high doses (best agent to raise HDL-C).
What adverse drug reactions could nicotinic acids produce?
Activation of peptic ulcer
Reduced insulin sensitivity
What are the contraindications for the use of nicotinic acid?
Active liver disease
Unexplained LFT elevations
Peptic ulcer disease
What is the mode of action of ezetimibe?
Selectively inhibits intestinal absorption of cholesterol - decreased intestinal delivery of cholesterol to the liver, increased expression of LDL receptors, decreased cholesterol content of atherogenic particles.
What adverse drug reactions can ezetimibe produce?
What does combination therapy involve?
Statin plus one of:
Fibrate (not gemfibrozil)