Cardio - lipid drugs

Question 1

What is the LDL target with moderate cardiovascular risk?

Answer 1

less than 3mM (115mg/dl)

Question 2

What is the LDL target with high cardiovascular risk?

Answer 2

less than 2,5mM (100 mg/dl)

Question 3

What is the LDL target with very high cardiovascular risk?

Answer 3

less than 1,8mM (70mg/dl)

Question 4

What is the mechanism of statins?

Answer 4

inhibition of HMG-CoA -> ldlR increase -> less LDL and also TGs

Question 5

Which of the statins are prodrugs?

Answer 5

Lovastatin and Simvastatin

Question 6

Which are the most potent statins? (3)

Answer 6

Pitavastatin, Rosuvastatin, Atorvastation, (Simvastatin)

Question 7

What are the toxicities of statins?

Answer 7

hepatotoxicity, myopathy, less glucose tolerance, teratogenicity, P450 interactions

Question 8

What are the pleiotrophic effects of statins? (3) (less isoprenylation)

Answer 8

less oxidative stress and vascular inflammation. Stabilization of atherosclerotic plaques.

Question 9

Whats is the mechanism of Ezetimibe

Answer 9

Selectivly inhibits intestinal cholesterol absorption (NPC1L1) -> less LDL

Question 10

What are the toxicities of Ezetimibe?

Answer 10

Hepatotoxicity, myopathy (rare)

Question 11

What is the mechanism of Colestipol, Cholestyramine, and Colesevelam?

Answer 11

Binding of bile in the intestine preventing absorption -> increased LDLreceptors -> less LDL

Question 12

What are the side effects of the bile binding resins?

Answer 12

constipation, bloating, diarrhea
less absoption of drugs and vitamins (ADEK)
unpleasant taste
formation of gallstones

Question 13

What is the mechanism of Fibrates:
gemfibrozil
fenofibrate
bezafibrate

Answer 13

increase in fatty acids oxidation in liver and muscles
increase lipoprotein lipase activity
inhibits lipase of adipose tissue
-> less LDL and TGs, increase HDL

Question 14

What are the toxicities of fibrates?

Answer 14

hepatotoxicity
myopathy (with statins)
formation of gallstones 
arrhythmias 
hypokalemia
GIT symptoms

Question 15

What is the mechanism of Niacin (nicotinic acid)

Answer 15

inhibits VLDL secretion
increases lipoprotein lipase activity
inhibits lipase of adipose tissue
-> less LDL and TGs, increased HDL

Question 16

What are the toxicities of Niacin?

Answer 16

flush (cutaneous vasodilation, PGD2)- use NSAIDs

nausea
hepatotoxicity
impaired glucose tolerance
hyperuricemia
arrhythmias

Question 17

What is the mechanism of
torcetrapib
anacetrapib
dalcetrapib

Answer 17

Cholesteryl ester transfer protein (CETP) inhibitors

-> increased HDL, less LDL

Question 18

Which lipid lowering drugs would you use in the treatment of hypercholesterolemia?

Answer 18

statin, resin, ezetimibe

Question 19

Which lipid lowering drugs would you use in the treatment of hypertriglyceridemia?

Answer 19

fibrate, niacin, omega-3

Question 20

Which lipid lowering drugs would you use in the treatment of combined hyperlipidemia?

Answer 20

statin/resin/ezetimibe + fibrate, niacin, omega-4

Question 21

Which lipid lowering drugs has the stronges LDL lowering action?

Answer 21

statins> ezetimibe, resins

Question 22

Which lipid lowering drugs has the strongest TG lowering action?

Answer 22

Fibrates, niacin, or strong statins

Question 23

Which lipid lowering drugs has the strongest increase on HDL?

Answer 23

Niacin > Fibrates

Question 24

What is the best life style interventions to reduce LDL?

Answer 24

Decrease intake of saturated fats and trans fat

Increase intake of dietary fibre and phyosterols

Question 25

What is the best life style interventions to reduce triglycerides?

Answer 25

Lose weight, less alcohol, reduce mono- and disaccharides

Question 26

What is the mechanism of action for omega-3?

Answer 26

inhibits VLDL and TG synthesis

4g daily reduces TGs by 25%