STATINS Flashcards
First-line for primary and secondary prevention
because of potency and cost-effectiveness
- Reduces major coronary events
- Reduces CHD mortality
- Reduces stroke
- Reduces total mortality
Statins, lowers cholesterol by 24-60%
Cholesterol lowering how?
- ↓ LDL by 24%-60%
- ↓ TG by 7%-30%
- ↑ HDL by 5%-15%
MOA
inhibit of HMG-CoA reductase
Most statins should be given in the _____?
evening
Exceptions: atorvastatin (Lipitor), rosuvastatin (Crestor)
All statins are metabolized by _____?
CYP enzymes
CYP3A4, CYP2C9, CYP2C19
High-intensity statin affect?
è lowers LDL by ≥ 50%
Moderate-intensity statin affect?
lowers LDL-C by 30% to < 50%
Low-intensity statin?
lowers LDL by <30%
Selection is based on _____?
patient’s ASCVD and indicated intensity
what high intensity statins have the greatest LDL lowering potential?
Atorvastatin 40-80 mg
Rosuvastatin 20-40 mg
what are the statins ADRs, the main one?
Hepatotoxicity***
muscle related ARs
Diabetes
Memory impairment
clinical presentation of statin OD?
contraindicated?
malaise, anorexia, dark- colored urine, yellowing of skin
active liver disease; in pregnancy, breast-feeding, and active liver disease
Muscle-related adverse reactions
- Myalgia
- Myopathy
- Myositis
- Rhabdomyolysis***
Drugs that reduce the catabolism of statins can increase the risk
Gemfibrozil
3A4 inhibitors
Extensive 3A4 metabolism, must be switched if combined with 3A4 inhibitor/inducer
Simvastatin, atorvastatin, lovastatin
Less/no 3A4 metabolism
Pravastatin, rosuvastatin, fluvastatin, so less risk of muscle injury and interactions when used with CYP3A4 inhibitors
most important effects of statins?
pleiotropic effects
increase plaque stabilization
decrease cholesterol, inflammation, platelet activation, increase NO bioactivity and endothelial fxn
