miargo17 LUpio-Lowering Agents: Lipidowering Agents This site is intended for healthcare professionals Medscape Lipid-Lowering Agents Updated: Mar 30, 2016 Author: Abimbola Farinde, PharmD, PhD; more... 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 htplemedicine medscape.conatle!2172172-overviow 12ranot7 Lipa-Lowering Agents: Lipd-Lowering Agents + 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, Apolipoprotein B antisense oligonucleotide These agents target messenger RNA for apolipoprotein B (apoB)-100, the principal apolipoprotein of LDL and its metabolic precursor, VLDL. Note the following + Reduces LDL, ApoB, total cholesterol (TC), and non-HDL cholesterol + Example includes Mipomersen + Contraindications include hypersensitivity, moderate-to-severe hepatic impairment or active liver disease including persistent increased levels of serum transaminases MTP inhibitor These agents directly bind and inhibit microsomal triglyceride transfer protein (MTP), thereby preventing ApoB-containing lipoproteins. Note the following: + Reduces LDL, TC, ApoB, and non-HCL cholesterol + Example includes Lomitapide + Contraindications include pregnancy, coadministration with strong CYP3A4 inhibitors (lomitapide exposure increased 27-fold), moderate-to-severe hepatic impairment or active liver disease including persistent increased levels of serum transaminases Omega 3 acids Omega 3 acids agents inhibit acyl CoA:1,2-diacylglycerol acyltransferase. Note the following: + Reduces non-HCL cholesterol, ratio of total cholesterol to HDL-C, VLDL, Apo-C, phospholipase A2, and arachidonic acid + Examples include Omega 3 fatty acids, omega 3 carboxylic acids, icosapent + Contraindications include hypersensitivity Combination Drugs These combination drugs lower lipids: Lovastatin and niacin (nicotinic acid) Atorvastatin and amlodipine Simvastatin and niacin Atorvastatin and ezetimibe Simvastatin and ezetimibe htplemedicine medscape.conatle!2172172-overviow 22