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Hypolipidemic Agents

This is a brief overview of hypolipidemic agents, or drugs that alter the levels of lipids in the body. I created this presentation with Google Slides. Image were created or taken from Wikimedia Commons I created this video with the YouTube Video Editor. ADDITIONAL TAGS Hypolipidemic Agents Statins Bile Acid Sequestrants Niacin Fibrates Statins Inhibit the enzyme HMG-CoA reductase, which is the rate limiting step in cholesterol synthesis Decrease LDL, increase HDL, decrease TGs Proven to reduce risk of coronary artery disease Side effects: Liver toxicity (most metabolized by cytochrome P450), muscle toxicity (rhabdomyolysis) Contraindications: liver disease, CYP450 inhibitor drugs, pregnancy (birth defects) Lovastatin, Pravastatin, Simvastatin, Atorvastatin, Rosuvastatin Statins Bile Acid Sequestrants Niacin Fibrates Bile Acid Sequestrants Binds bile acid in the gut and prevents reuptake, thus promoting excretion of bile acid Cholesterol is typically converted to bile acid and secreted into the GI tract; 99% of this bile acid is then reabsorbed into the body Loss of 1% of bile acid is typically the only method of removing cholesterol from the body Bile acid sequestrants allow for more than 1% of bile acid to excreted from the body, forcing body to produce more bile acid from cholesterol Decrease LDL, increase HDL, no effect on TGs Side effects: GI distress (nausea, constipation, bloating → since it’s inhibiting fat absorption, resolved with fiber intake) Malabsorption of other drugs and fat-soluble vitamins (DEAK) Avoid use in people with familial dysbetalipoproteinemia with very high TG Colestipol (Colestid), Colesevelam (Welchol), Cholestyramine (Questran) Statins Bile Acid Sequestrants Niacin Fibrates Niacin Prevents release of free fatty acid into the bloodstream from adipocytes Increases HDL by decreasing hepatic excretion of a major protein in HDL (apoA-I) Increase HDL, decreases LDL, decreases TGs Side effects: skin flushing (resolved with aspirin), hyperuremia, hyperglycemia, GI distress (n/v and peptic ulcers), and hepatotoxicity Contraindications: patients with gout and liver disease (monitor liver enzymes) Niacin (Niaspan, Niacor) is also known as nicotinic acid or vitamin B3 Niacin has a number of other functions, and lack of niacin causes pellagra, degenerative disease causing skin lesions (shown) and mental disturbance Statins Bile Acid Sequestrants Niacin Fibrates Fibrates Activate a transcription factor (peroxisome proliferator-activated receptors (PPARs)) that increases lipoprotein lipase, which converts VLDL to LDL and therefore reduces VLDL and triglyceride levels PPARs are regulators that transport from cytoplasm to nucleus to bind regulatory regions of target genes Decrease TGs, decrease LDL, increase HDL Side effects: GI distress, skin rash, muscle toxicity (also worsened by statins, too), hypokalemia, arrhythmias Avoid use in patients with liver and renal disease Gemfibrozil Fenofibrate Statins Bile Acid Sequestrants Niacin Fibrates