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Anti-Hypercholesterolemic Agents PowerPoint PPT Presentation


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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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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


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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%.

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Lipoprotein Particles

Structure

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Transport of Lipoprotein Particles

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Lipoprotein Particles

Classification of lipoprotein particles

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Hyperlipidemia

Types of hyperlipidemias

N = normal, = increase; = decrease; = slight increase; = slight decrease

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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

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R

R

R

R

Anti-hyperlipidemic Drugs - Statins

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Anti-hyperlipidemic Drugs - Statins

Atorvastatin Cerivastatin Fluvastatin

Rosuvastatin Pitavastatin

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HMG CoA substrate

For example,

Mevastatin

Lovastatin

Simvastatin

For example,

Fluvastatin

Atorvastatin

Cerivastatin

Anti-hyperlipidemic Drugs - Statins

Rationale – competitive binding

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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.

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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

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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

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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

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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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