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CHAPTER 29

CHAPTER 29. Hypolipidemic Drugs. Danger – Heart attack. Coronary heart disease causes ½ of all deaths in USA Caused by: Elevated low density lipoproteins ( ↑ LDL) Elevated triglycerides (  TG) Decreased high density lipoproteins ( ↓ HDL)

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CHAPTER 29

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  1. CHAPTER 29 Hypolipidemic Drugs

  2. Danger – Heart attack • Coronary heart disease causes ½ of all deaths in USA • Caused by: • Elevated low density lipoproteins (↑ LDL) • Elevated triglycerides (  TG) • Decreased high density lipoproteins (↓ HDL) • Reduction of the LDL level is the primary goal of cholesterol-lowering therapy

  3. Clinical Indication Adjunct therapy to reduce elevated cholesterol especially in patients with elevated low density lipoproteins (LDL) who do not respond to dietary adjustment Prevent the progression of coronary atherosclerosis in coronary heart disease Prevent the risk of death from acute coronary episodes

  4. Lipoproteins Are produced in liver and intestines to transport lipids (fats) such as • cholesterol • triglycerides Vary in density from • Very low density (VLDL) • Low density (LDL) involved in atherosclerosis • High density (HDL) cardioprotective

  5. Risk Factors Associated with Coronary Heart Disease • Age Men > 45 yrs Women > 55 yrs • History of Smoking • Hypertension Antihypertension medications Premature menopause Obesity • Hormone imbalance Diabetes mellitus • Low HDL, high LDL levels

  6. Hypolipdemic Drugs Bile acid sequestrants (binders) cholestyramine, colestipol HMG-CoA Reductase Inhibitors block cholesterol synthesis atrovastatin, cervastatin, lovastatin, pravastatin, simastatin Alter lipid and lipoprotein metabolism clofibrate, dextrothyroxine, gemfibrozil, niacin

  7. Bile acid sequesterants • Bind bile acids and cholesterol in bowel and deplete body pool - liver removes more LDL from blood to synthesize more bile salts – Hence lowers blood level of LDL • Cholestyramine (Questran) • Colestipole (Colestid)

  8. HMG-CoA reductase inhibitors • This enzyme is the rate-limiting step in hepatic synthesis of cholesterol • Note: serum cholesterol – 1/3 dietary, 2/3 synthesized by liver • Lowers VLDL,LDL & triglyceride • Raises HDL • Lovastatin (Mevacor) • Atrovastatin (Lipitor)

  9. Adverse Effects of HMG-CoA Reductase Inhibitors • Elevated serum liver enzymes (AST, ALT) • Muscle aches • Muscle weakness • Elevate serum creatine phosphokinase (CPK) • Headache • Dizziness • Diarrhea • Abdominal cramping, flatulence • Alteration of taste

  10. Fibric Acids • Increases the uptake of fat by fat cells from VLDL and chylomicrons by activating lipoprotein lipase – lowers cholesterol & TG • Gemfibrozil (Lopid) • Fenofibrate (Tricor)

  11. Nicotinic Acid • Inhibits lipolysis and release of fatty acids in fat cells – lowers synthesis of triglycerides by liver – lowers VLDL & LDL • Niacin (Niacor)

  12. Cholesterol Absorption Inhibitors • Acts at mucosal surface of the small bowel to block absorption of dietary cholesterol • Ezetimibe (Zetia) • Problems: • Most cholesterol is not dietary • Foul smelling stools • Blocks fat soluble vitamins (A,D,E,K)

  13. Contraindications HMG-CoA Reductase Inhibitors Patients who have • Acute liver disease • Hypersensitivity • Persistent elevation in serum liver enzymes Pregnancy Patients using gemfibrozil because severe cardiomyopathy may develop Dextrothyroxine Patients with angina, myocardial infarction, arrhythmias, congestive heart failure Pregnancy

  14. Drug Interactions HMG-CoA Reductase Inhibitors Competition for liver enzymes, increase levels • Alcohol, antifungal drugs, digoxin, warfarin Decrease HMG-CoA Inhibitor levels • Nicotinic acid, propranolol Dextrothyroxine • Increase bleeding with anticoagulants • Block antidiabetic drugs, increase serum glucose Bile Acid Sequestrants Bind fat soluble vitamins, drugs to reduce absorption • Vitamins A, D, K • Anticoagulants, aspirin, furosemide, glipizide, methyldopa

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