Lipid lowering drugs
Posted: 25 May 2012, 17:12
The mode of action of fibrates is to enhance lipoprotein lipase activity, increase low-density lipoprotein (LDL) receptor-mediated clearance of LDL and increase high-density lipoprotein (HDL) synthesis. This leads to a corresponding fall in triglycerides due to a fall in very low-density lipoprotein (VLDL), and a rise in HDL. In total, they reduce triglycerides by 20–60%, LDL by 5–25%, and increase HDL by 15–30%. Statins are inhibitors of hydroxymethylglutaryl-CoA (HMG-CoA) activity (the rate-limiting step in cholesterol synthesis), niacin predominantly inhibits adipocyte lipolysis, and resins like cholestyramine are responsible for binding of bile acids in the gut. Inhibitors of CETP are currently in clinical trials as anti-atherosclerotic agents in patients with dyslipidaemia