hyperlipidemia drugs Flashcards
Pro-atherogenic effects of Ox-LDL
Inhibits macrophage motility
• Induces T-cell activation and VSMC division /
differentiation
- Toxic to endothelial cells
- Enhances platelet aggregation
Old Classes of Lipid Lowering Drugs
● Statins - simvastatin
● Cholesterol lipase inhibitors - ezetimibe
● Nicotinic acid / niacin
● Fibrates – fenofibrate
● Resins - colestyramine
● Omega-3 fatty acids - omacor
● ? Plant sterols
which drug class doesnt have much of systemic effects and why?
Ezetimibe and its active glucuronide metabolite
bc they circulate enterohepatically
• Delivers agent back to the site of action
• Limits systemic exposure
Statins
Mechansim of action of statins
Adverse Drug Reactions of Statins
• Increased transaminase levels
• 0.1%-2.5% of treated patients develop increases of >
3 x upper-normal limit, especially at higher doses
• Rapidly reversible, no evidence of chronic liver disease
• Myopathy
- Diffuse muscle pain and CPK > 10 x upper-normal limit
- Primarily seen when higher doses of statins are used in combination with cyclosporine, gemfibrozil, and occasionally erythromycin and niacin
• Miscellaneous
• Gastrointestinal complaints, arthralgias, and headaches
Some secondary benefits of Statin treatment
Anti-inflammatory
●Plaque reduction
● Improved endothelial cell function
● Reduced thrombotic risk
decreases endothelin>> which causes vasoconstriction
Statin therapy is recommended as part of the management strategy for who?
for the primary prevention of CVD for adults who have a 20% or greater 10-year risk of developing CVD.
which statin is now withdrawn from the market?
Cerivastatin >> causes drug0drug interaction due to reports of fatal rhabdomyolysis.
Mechanism of action of fibric acids and side effects
mainly to reduce TAG!
SE:
GI upset (8%), cholelithiasis, myositis,
AbnormL LFTs
changing ur diet has a greater impact on which lipids in the body?
TAG is modified much more easily than cholestrol!
Fibric Acid Derivatives
Indications, Efficacy , Side Effects, Contraindications:
Nicotinic Acid
- Adverse effects,
- Contraindications
indication
how do we reduce side effects of niacin>> Flushing, itching, headache ?
reduced by immediate-release, Niaspan® or combination with low-dose aspirin
Ezetimibe: Mechanism of Action