Cholestin (dietary supplement made from red yeast) Mechanism of Action Inhibits the enzyme (HMG-CoA) that synthesizes cholesterol Increases the number of LDL receptors on liver cells to remove more LDL Decreases production of VLDLs and raises HDL levels Stabilizes plaque, slows progression of coronary calcification Improves endothelial function Enhances the ability of blood vessels to dilate Reduces the risk of thrombosis Inhibits platelet deposition and aggregation May increase bone formation Uses Hypercholesterolemia Primary and secondary prevention of CV events Post MI therapy Prevention of CV events in people with diabetes Adverse Effects Headache, rash, GI complaints Myopathy, increases CK levels, rhabdomyolysis, dark urine, renal failure Hepatotoxicity, increases ALT and AST Rare peripheral neuropathy Pregnancy risk Category X Possible effects on cognition Possible hyperglycemia Drug Interactions Macrolide antibiotics, azole antifungals HIV protease inhibitors, amiodarone, cyclosporine, and grapefruit juice raise some statins to toxic levels 19
Ch 50: Prophylaxis of Coronary Heart Disease: Drugs That Help Normalize Cholesterol and Triglyceride Levels NICOTINIC ACID Prototype: Nicotinic Acid (Niacor, Niaspan) Drug Combinations Lovastatin/niacin (Advicor) Simvastatin/niacin (Simcor) Mechanism of Action Reduces LDL and triglycerides Increases HDL Uses Lowers triglycerides in patients at risk for pancreatitis Dyslipidemia Reduces the risk of major coronary events Reduces total mortality Adverse Effects Flushing and itching (take 325 mg ASA 30 minutes before dose) Gastric upset, nausea, vomiting, diarrhea Hepatotoxicity May raise blood sugar in patients with diabetes May increase incidence of gout 20
Ch 50: Prophylaxis of Coronary Heart Disease: Drugs That Help Normalize Cholesterol and Triglyceride Levels BILE-ACID SEQUESTRANTS Prototype: Colesevelam (Welchol) Other Agents Cholestyramine (Questran) Colestipol (Colestid) Mechanism of Action Binds (sequesters) bile acids in the GI tract Prevents the absorption and promotes their excretion Forms insoluble complex with bile acids Increases LDL receptors Safest of all lipid-lowering drugs Uses Hypercholesterolemia Often used in combination with statin Approved to control hyperglycemia in patients with type 2 diabetes Adverse Effects Constipation, bloating, indigestion Interferes with absorption of other drugs May impede absorption of fat-soluble vitamins 21
Ch 50: Prophylaxis of Coronary Heart Disease: Drugs That Help Normalize Cholesterol and Triglyceride Levels EZETIMIBE (Zetia) Cholesterol-Lowering Drug Drug Combinations Simvastatin/ezetimibe (Vytorin) Mechanism of Action Inhibits cholesterol absorption in the small intestine Reduces LDL, triglycerides, and apolipoprotein B Small increase in HDL Uses Hypercholesterolemia Used in combination with statins Adverse Effects Reports of myopathy, rhabdomyolysis, pancreatitis, and thrombocytopenia May increase risk of liver damage when used with statins 22
Ch 50: Prophylaxis of Coronary Heart Disease: Drugs That Help Normalize Cholesterol and Triglyceride Levels
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- Spring '14
- Cardiology, adverse effects