Cardio - lipid drugs Flashcards
What is the LDL target with moderate cardiovascular risk?
less than 3mM (115mg/dl)
What is the LDL target with high cardiovascular risk?
less than 2,5mM (100 mg/dl)
What is the LDL target with very high cardiovascular risk?
less than 1,8mM (70mg/dl)
What is the mechanism of statins?
inhibition of HMG-CoA -> ldlR increase -> less LDL and also TGs
Which of the statins are prodrugs?
Lovastatin and Simvastatin
Which are the most potent statins? (3)
Pitavastatin, Rosuvastatin, Atorvastation, (Simvastatin)
What are the toxicities of statins?
hepatotoxicity, myopathy, less glucose tolerance, teratogenicity, P450 interactions
What are the pleiotrophic effects of statins? (3) (less isoprenylation)
less oxidative stress and vascular inflammation. Stabilization of atherosclerotic plaques.
Whats is the mechanism of Ezetimibe
Selectivly inhibits intestinal cholesterol absorption (NPC1L1) -> less LDL
What are the toxicities of Ezetimibe?
Hepatotoxicity, myopathy (rare)
What is the mechanism of Colestipol, Cholestyramine, and Colesevelam?
Binding of bile in the intestine preventing absorption -> increased LDLreceptors -> less LDL
What are the side effects of the bile binding resins?
constipation, bloating, diarrhea
less absoption of drugs and vitamins (ADEK)
unpleasant taste
formation of gallstones
What is the mechanism of Fibrates:
gemfibrozil
fenofibrate
bezafibrate
increase in fatty acids oxidation in liver and muscles
increase lipoprotein lipase activity
inhibits lipase of adipose tissue
-> less LDL and TGs, increase HDL
What are the toxicities of fibrates?
hepatotoxicity myopathy (with statins) formation of gallstones arrhythmias hypokalemia GIT symptoms
What is the mechanism of Niacin (nicotinic acid)
inhibits VLDL secretion
increases lipoprotein lipase activity
inhibits lipase of adipose tissue
-> less LDL and TGs, increased HDL
What are the toxicities of Niacin?
flush (cutaneous vasodilation, PGD2)- use NSAIDs
nausea hepatotoxicity impaired glucose tolerance hyperuricemia arrhythmias
What is the mechanism of
torcetrapib
anacetrapib
dalcetrapib
Cholesteryl ester transfer protein (CETP) inhibitors
-> increased HDL, less LDL
Which lipid lowering drugs would you use in the treatment of hypercholesterolemia?
statin, resin, ezetimibe
Which lipid lowering drugs would you use in the treatment of hypertriglyceridemia?
fibrate, niacin, omega-3
Which lipid lowering drugs would you use in the treatment of combined hyperlipidemia?
statin/resin/ezetimibe + fibrate, niacin, omega-4
Which lipid lowering drugs has the stronges LDL lowering action?
statins> ezetimibe, resins
Which lipid lowering drugs has the strongest TG lowering action?
Fibrates, niacin, or strong statins
Which lipid lowering drugs has the strongest increase on HDL?
Niacin > Fibrates
What is the best life style interventions to reduce LDL?
Decrease intake of saturated fats and trans fat
Increase intake of dietary fibre and phyosterols
