drugs for lipid lowering agents Flashcards
why is HDL anti-atherogenic?
- reverse cholesterol transport
- protects against endothelial dysfunction
- inhibits oxidative stress
what are the 5 classes of hypolipidemic agents?
- nicotinic acid (niacin)
- fibric acid derivatives (fibrates)
- bile acid sequestrants (resins)
- HMG-CoA reductase inhibitors (statins)
- Ezetimibe (a new class of lipid lowering agent)
what does niacin do?
- raises HDL
- lowers TGs
- lowers LDL
side effects of niacin?
- hepatoxicity
- hyperglycemia
- hyperuricemia
- flushing
- pruritis
- dyspepsia
- rashes
what does fibric acid derivatives do?
- reduction in VLDL
- variable (but small) effects on LDL
- 10% increase in HDL
what is the mech of fibrates?
effects are mediated by binding to PPARa
how does gemfibrozil work?
activation of lipoprotein lipase
what are bile acid sequestrants (resins)?
- anion-exchange resins that bind bile acids in the intestines
- are not absorbed, bound bile acids secreted in stool
- decreases LDL but increases TGs
- safe, but interferes with absorption of fat-soluble vitamines
what are statins?
- most effective, best-tolerated
- reduce LDL, VLDL
- increase HDL
what are the adverse effects of statins?
- hepatic dysfunction
2. myopathy
what are the two possible beneficial effects of statins?
- counteract osteoporosis
2. cardioprotective
what is the new class of lipid lowering agent?
ezetimibe
what is the mech of ezetimibe?
inhibits both dietary and biliary cholesterol absorption in the intestine by blocking a sterol transporter on the enterocyte –> thus, it reduces the amount of cholesterol delivered to the liver
what are the effects of ezetimibe?
- lowers LDL (synergistic with statins)
- once a day pill
- few side effects
both ezetimibe and simvastatin lowered LDL
by 52% at the starting dose
