STATINS

Question 1

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

Answer 1

Statins, lowers cholesterol by 24-60%

Question 2

Cholesterol lowering how?

Answer 2

• ↓ LDL by 24%-60%
• ↓ TG by 7%-30%
• ↑ HDL by 5%-15%

Question 3

MOA

Answer 3

inhibit of HMG-CoA reductase

Question 4

Most statins should be given in the _____?

Answer 4

evening

Exceptions: atorvastatin (Lipitor), rosuvastatin (Crestor)

Question 5

All statins are metabolized by _____?

Answer 5

CYP enzymes

CYP3A4, CYP2C9, CYP2C19

Question 6

High-intensity statin affect?

Answer 6

è lowers LDL by ≥ 50%

Question 7

Moderate-intensity statin affect?

Answer 7

lowers LDL-C by 30% to < 50%

Question 8

Low-intensity statin?

Answer 8

lowers LDL by <30%

Question 9

Selection is based on _____?

Answer 9

patient’s ASCVD and indicated intensity

Question 10

what high intensity statins have the greatest LDL lowering potential?

Answer 10

Atorvastatin 40-80 mg

Rosuvastatin 20-40 mg

Question 11

what are the statins ADRs, the main one?

Answer 11

Hepatotoxicity***
muscle related ARs
Diabetes
Memory impairment

Question 12

clinical presentation of statin OD?

contraindicated?

Answer 12

malaise, anorexia, dark- colored urine, yellowing of skin

active liver disease; in pregnancy, breast-feeding, and active liver disease

Question 13

Muscle-related adverse reactions

Answer 13

• Myalgia
• Myopathy
• Myositis
• Rhabdomyolysis***

Question 14

Drugs that reduce the catabolism of statins can increase the risk

Answer 14

Gemfibrozil

3A4 inhibitors

Question 15

Extensive 3A4 metabolism, must be switched if combined with 3A4 inhibitor/inducer

Answer 15

Simvastatin, atorvastatin, lovastatin

Question 16

Less/no 3A4 metabolism

Answer 16

Pravastatin, rosuvastatin, fluvastatin, so less risk of muscle injury and interactions when used with CYP3A4 inhibitors

Question 17

most important effects of statins?

Answer 17

pleiotropic effects

increase plaque stabilization
decrease cholesterol, inflammation, platelet activation, increase NO bioactivity and endothelial fxn