(From Baby Katzung and lecture, 5 Feb 2001, by Brian Buschman)
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Lovastatin and simvastatin are CoA analogs that block the production of cholesterol. This causes the liver to produce more LDL receptors which take up more lipid. This lowers plasma lipid by putting it into the liver.
Lovastatin and simvastatin are prodrugs but the rest of the class are already in the active form. They are used for lowering cholesterol and triglycerides levels. Sometimes adverse affects include a light rise in aminotransferases but usually there are few adverse affects.
Colestyramine is a bile-acid binding resin that is not absorbed from the gut. In the gut it exchanges Cl- for bile acids thereby preventing their reabsorption. This in turn causes increased bile acid production. Since the liver makes bile acids from cholesterol it lowers plasma LDL levers.
Adverse effects are limited o bloating, constipation and impaired absorption of some acidic and neutral drugs. It is unable to have too many adverse affects since it is never absorbed into the body.
Niacin is a vitamin that when taken reduces the hepatic synthesis of cholesterol. LDL and VLDL go down and HDL goes up. It’s common side effect is flush from increased prostaglandins. This can be prevented by pretreatment with NSAIDs. Tolerance to the flush comes quickly.
Gemfibrozil stimulates lipolysis peripherally thereby causing a reduction in triglycerides levels. Again, adverse affects include intestinal problems. Newer drugs in this class like clofibrate have more toxic effects including myalgia.
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