Lipid Lowering Agents

Lipid-Lowering Agents HMG-CoA reductase inhibitors (statins) These agents inhibit the rate-limiting step in cholesterol biosynthesis by competitively inhibiting HMG-CoA reductase. Note the following: Low-density lipoprotein (LDL) reduction of 25%-60% Examples include Atorvastatin, fluvastatin, lovastatin, pitavastatin, pravastatin, rosuvastatin, simvastatin Contraindications include hypersensitivity, active liver disease, pregnancy, lactation, coadministration with strong CYP3A4 inhibitors (selected statins) Vitamin B3 Vitamin B3 inhibits very-low-density lipoprotein (VLDL) synthesis. Note the following: LDL reduction of 10% High-density lipoprotein (HDL) increase of 20% Example includes Niacin (nicotinic acid) Contraindications include hypersensitivity, liver disease, active peptic ulcer, severe hypotension, arterial bleeding Fibrates Fibrates enhance lipoprotein lipase, resulting in increased VLDL catabolism, fatty acid oxidation, and triglycerides elimination. They decrease hepatic extraction of free fatty acids. Note the following: LDL reduction of 15% Triglyceride reduction of 35% Examples include Gemfibrozil, fenofibrate, fenofibrate (micronized), fenofibric acid Contraindications include active liver disease, renal disease, primary biliary cirrhosis, gallbladder disease 2-Azetidiones These agents inhibit sterol transporter at brush border and, consequently, intestinal absorption of cholesterol. LDL reduction of 15% Example includes Ezetimibe Contraindications include hypersensitivity, coadministration with statins (if active liver disease) Bile acid sequestrants These agents lower cholesterol and LDL via bile duct sequestration. Note the following: LDL reduction of 15% Examples include Cholestyramine, colesevelam, colestipol Contraindications include biliary/bowel obstruction, serum triglycerides >300-500 mg/dL, history of hypertriglyceridemia-induced pancreatitis