This is a brief overview of hypolipidemic agents, or drugs that alter the levels of lipids in the body.

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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