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Anti-Hypercholesterolemic Agents

Anti-Hypercholesterolemic Agents. Biosynthesis and Metabolism of Cholesterol What is arteriosclerosis? - Link between arteriosclerosis and cholesterol Lipoproteins particles - Structure and classification of lipoprotein particles Hyperlipidemias

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Anti-Hypercholesterolemic Agents

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  1. Anti-Hypercholesterolemic Agents • Biosynthesis and Metabolism of Cholesterol • What is arteriosclerosis? - Link between arteriosclerosis and cholesterol • Lipoproteins particles - Structure and classification of lipoprotein particles • Hyperlipidemias - Types and overall strategy to control hyperlipidemias • Anti-hyperlipidemic Agents - Classes • Statins • Fibrates • Bile Acid Sequestrants • Nicotinic Acid • Ezetimibe MEDC 603 Steroids

  2. Arteriosclerosis Arteriosclerosis is excessive formation and deposition of endogeneous products from blood. In 1984 a 1% drop in serum cholesterol was found to reduce the risk to coronary heart disease (CHD) by nearly 2%. MEDC 603 Steroids

  3. Lipoprotein Particles Structure MEDC 603 Steroids

  4. Transport of Lipoprotein Particles MEDC 603 Steroids

  5. Lipoprotein Particles Classification of lipoprotein particles MEDC 603 Steroids

  6. Hyperlipidemia Types of hyperlipidemias N = normal, = increase; = decrease; = slight increase; = slight decrease MEDC 603 Steroids

  7. Biosynthesis Diet LDL-R Cellular Cholesterol Serum Cholesterol Conversion to hormones within cells or storage as granules Bile Acids Re-absorption Intestine Lipoprotein catabolism Feces Strategy for Controlling Hyperlipidemia STATINS HMG CoA reductase Ezetimibe BILE ACID SEQUESTRANTS FIBRATES MEDC 603 Steroids

  8. R R R R Anti-hyperlipidemic Drugs - Statins MEDC 603 Steroids

  9. Anti-hyperlipidemic Drugs - Statins Atorvastatin Cerivastatin Fluvastatin Rosuvastatin Pitavastatin MEDC 603 Steroids

  10. HMG CoA substrate For example, Mevastatin Lovastatin Simvastatin For example, Fluvastatin Atorvastatin Cerivastatin Anti-hyperlipidemic Drugs - Statins Rationale – competitive binding MEDC 603 Steroids

  11. Anti-hyperlipidemic Drugs - Statins Pharmacokinetic properties of statins – case of cerivastatin Typically all statins possess side effects. The most dominant side effect, cited in the withdrawal of cerivastatin, is rhabdomyolysis (lysis of rhabdomyose) or weakening of skeletal muscles. MEDC 603 Steroids

  12. Anti-hyperlipidemic Drugs - Fibrates • Older generation drugs; introduced in 1981 • Second most useful anti-hyperlipidemic drugs • Primarily decrease serum triglycerides • Increase lipoprotein catabolism; increase TG usage by the body • Most used in Type III, IV and V hyperlipidemias MEDC 603 Steroids

  13. Anti-hyperlipidemic Drugs – Bile Acid Sequestrants • Anion exchange resins • Water insoluble and inert to digestive enzymes • Not absorbed through the GI tract • Positively charged nitrogens sequester bile acid re-absorption • Lower serum LDL levels • Most useful in type IIa and IIb hyperlipidemias MEDC 603 Steroids

  14. Anti-hyperlipidemic Drugs – Nicotinic Acid • Administered in large doses (0.5 to 6 grams daily) • Reduces triglycerides and total cholesterol • Increases biliary secretion of cholesterol, but not bile acids • Useful in Type IIa, IIb, III, IV and V hyperlipidemias MEDC 603 Steroids

  15. Anti-hyperlipidemic Drugs – Ezetimibe • Approved in October 2002 • Reduces serum LDL, TC, and TG and increases HDL • Prevents the absorption of cholesterol from diet • Useful in Type IIa, IIb, III, IV and V hyperlipidemias MEDC 603 Steroids

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