Anti-Hyperlipidemic Agents

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HMG-COA Inhibitors

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Lovastatin

"Statins"

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Bile Acid Binding Resins

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Cholestyramine

"Resins"

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VLDL Secretion Inhibitors

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Niacin (Vitamin B3)

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Fibric Acid Derivatives

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Gemfibrozil

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Intestinal Sterol Absorption Inhibitors

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Ezetimibe

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MoA of Lovastatin

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Works in the cytosol of the liver --> competitively inhibits HMG-CoA reductase (the RLS of cholesterol synthesis (HMG-CoA --> mevalonic acid) in the liver), causing an upregulation of LDL receptors which leads to increased extraction of exogenous LDL from the blood and a reduction of hepatic VLDL production

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Therapeutic Uses of Lovastatin

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DOC for all hyperlipidemias, especially those with high LDL; atherosclerosis, primary prevention of coronary artery disease and stroke

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AE of Lovastatin

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GI: nausea, abdominal pain, constipation, flatulence (common @ beginning of therapy); increase in serum aminotransferase, hepatotoxicity;
Myopathy and rhabdomyolysis

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CI of Lovastatin

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PREGNANCY; concurrent use of niacin, fibrates, and drugs that inhibit CYP enzymes; hepatic disease, jaundice, cholestasis, alcoholism

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MoA of Cholestyramine

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0% bioavailability; stays in GI lumen and picks up bile in exchange for Cl --> no bile available for endogenous LDL synthesis causing an upregulation of LDL receptors which leads to increased extraction of exogenous LDL from the blood and increased cholesterol synthesis to make new bile

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Therapeutic Uses of Cholestyramine

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Only hyperlipidemias with increased LDL; itching associated with cholestasis; diarrhea

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AE of Cholestyramine

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Constipation; hypertriglyceridemia; metabolic acidosis; decreased intestinal absorption of fat soluble vitamins and many drugs (WARFARIN)

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CI of Cholestyramine

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Severe hypertriglyceridemia; any pre-existing coagulopathy (due to decreased absorption of Vit.K); constipation; cholelithiasis, biliary obstruction, biliary cirrhosis

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MoA of Niacin

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Strongly inhibits lipolysis in adipose tissue which leads to a reduction of triglycerides, decreased synthesis & secretion of VLDL --> reduction of LDL, increased HDL;
Other effects: reduction of fibrinogen levels (improvement of atherosclerosis & thrombosis); stimulation of PG production and histamine release; inhibition of uric acid secretion; decreased glucose tolerance

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Therapeutic Uses of Niacin

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All hyperlipidemias involving increased VLDL & LDL, and decreased HDL

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AE of Niacin

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Intense cutaneous flush (can be prevented by NSAID prophylaxis); hepatotoxicity; rhabdomyolysis (if given with a STATIN); drug should be discontinued if aminotransferase levels are elevated to more than 3x normal limits

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CI of Niacin

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Peptic ulcer disease (due to histamine release); diabetes; gout & hyperuricemia; bleeding & coagulopathy (decreased fibrinogen)

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MoA of Gemfibrozil

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Activation of nuclear transcription receptor PPARalpha, mainly in the liver and brown adipose tissue --> increase synthesis of lipoprotein lipase and enhanced hydrolysis of VLDL, therefore decreased plasma VLDL

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Therapeutic Uses of Gemfibrozil

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DOC for Type 3 hyperlipoproteinemia; hypertriglyceridemias

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AE of Gemfibrozil

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Myopathy & rhabdomyolysis (if given with a STATIN); cholelithiasis; dysgeusia, nausea, abdominal pain, diarrhea

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CI of Gemfibrozil

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Gallbladder disease, biliary cirrhosis, hepatic disease

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MoA of Ezetimibe

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Localizes at the brush border of small intestine and selectively inhibits the intestinal absorption of cholesterol and related sterols; also reduces Apo-B

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Therapeutic Uses of Ezetimibe

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Hyperlipidemias, most often with a statin (SYNERGISTIC - additional 25% reduction than with statins alone)

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AE of Ezetimibe

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No increase in myopathy frequency when given with statins; myalgia, diarrhea

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CI of Ezetimibe

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Severe hepatic disease (half-life of drug is prolonged!!)