Drugs for Lipid Disorders 16 Drugs for Lipid Disorders

Directory Classroom Response System Lecture Note Presentation

Question 1 The patient has developed gallstones and elevated liver enzymes. Which of the following cholesterol-lowering medications could cause this?

Question 1 Choices Cholestyramine (Questran) Niacin (Nicotinic acid) Gemfibrozil (Lopid) Lovastatin (Mevacor)

Question 1 Answer Cholestyramine (Questran) Niacin (Nicotinic acid) Gemfibrozil (Lopid) Lovastatin (Mevacor)

Question 2 The preferred first-choice drugs to treat elevated cholesterol levels are:

Question 2 Choices Statins Bile acids Fibric acids Nicotinic acids

Question 2 Answer Statins Bile acids Fibric acids Nicotinic acids

Question 3 Statin drugs are most effective when administered:

Question 3 Choices In the morning In the evening With other medications On an empty stomach

Question 3 Answer In the morning In the evening With other medications On an empty stomach

Question 4 When asked how an HMG-CoA reductase inhibitor lowers cholesterol, the nurse correctly answers that it is by inhibiting the manufacture of cholesterol or by:

Question 4 Choices Increasing the secretion of bile acids Decreasing triglyceride production Removing cholesterol from the small intestine Promoting the breakdown of cholesterol

Question 4 Answer Increasing the secretion of bile acids Decreasing triglyceride production Removing cholesterol from the small intestine Promoting the breakdown of cholesterol

Learning Outcomes Summarize the link between high blood cholesterol, LDL levels, and cardiovascular disease. Compare and contrast the different types of lipids. Illustrate how lipids are transported through the body.

Learning Outcomes Compare and contrast the different types of lipoproteins. Give examples of how blood lipid levels can be controlled through nonpharmacological means.

Learning Outcomes For each of the classes in the Drug Snapshot, identify representative drugs, explain their mechanisms of action, primary actions, and important adverse effects: Categorize antilipidemic drugs based on their classifications and mechanisms of action.

High blood lipid levels can lead to cardiovascular disease. Core Concept 16.1 High blood lipid levels can lead to cardiovascular disease.

High Cholesterol The greater the amount of cholesterol circulating in the blood, the greater the risk of cardiovascular disease. Circulating cholesterol bind to vessel walls, increasing plaque buildup as years pass.

Figure 16.1 Chemical structures of the three classes of lipids: (a) triglycerides, (b) phospholipids, (c) steroids

Core Concept 16.2 The three classes of lipids are triglycerides, steroids, and phospholipids.

Figure 16.2 Composition of lipoproteins: (a) HDL; (b) LDL; (c) VLDL

Lipoprotein levels are important predictors of cardiovascular disease. Core Concept 16.3 Lipoprotein levels are important predictors of cardiovascular disease.

Lipid levels can often be controlled through lifestyle changes. Core Concept 16.4 Lipid levels can often be controlled through lifestyle changes.

Therapeutic Lifestyle Changes Increase physical activity, which raises HDL levels and lowers triglycerides Maintain optimum weight because obesity is a major risk factor for coronary heart disease Reduces dietary saturated fat to 7% of total caloric intake

Therapeutic Lifestyle Changes Reduces cholesterol intake to less than 200 mg/day Increases intake of whole grains, vegetables, and fruits so that total dietary fiber is 10 to 25 g/day Reduce or eliminate tobacco use.

Concept Review 16.1 Why is the cholesterol in high-density lipoproteins considered to be “good” cholesterol?

Statins are drugs of choice in reducing blood lipid levels. Core Concept 16.5 Statins are drugs of choice in reducing blood lipid levels.

Statins Revolutionized the treatment of lipid disorders.

Statins Effects Dramatic 20%-40% reduction in LDL-cholesterol levels Decrease LDL-cholesterol levels in the blood Lower triglyceride levels Lower VLDL levels Raise “good” HDL-cholesterol levels. Reduce the incidence of serious cardiovascular related events by 25% to 30%.

Statins Act by inhibiting HMG-CoA reductase.

Figure 16.3 Cholesterol biosynthesis and excretion

Table 16.2 (continued) Drugs for Dyslipidemias

Bile acids can increase cholesterol excretion and reduce LDL levels. Core Concept 16.6 Bile acids can increase cholesterol excretion and reduce LDL levels.

Bile acids Substances that aid the digestion of fats, Once bound in the intestine, the cholesterol in the bile acids is eliminated in the feces

Bile acids No longer considered first-line drugs for hyperlipidemia Sometimes combined with statins for patients who are unable to achieve sufficient response from the statins alone

Nicotinic acid can reduce triglyceride and LDL-cholesterol levels. Core Concept 16.7 Nicotinic acid can reduce triglyceride and LDL-cholesterol levels.

Nicotinic Acid (niacin) Water-soluble B-complex vitamin primary action is to decrease VLDL levels Also reduction in LDL-cholesterol and triglyceride Reduces triglycerides and increases HDL levels.

Concept Review 16.2 How does the mechanism of the statins differ from that of nicotinic acid?

Core Concept 16.8 Fibric acid agents lower triglyceride levels but have little effect on LDLs.

Fibric Acid Agents, or Fibrates Largely replaced by the statins Sometimes used in combination with the statins. Drugs of choice for treating extremely high triglyceride levels

Figure 16.4 Mechanisms of action of lipid-lowering drugs

Core Concept 16.9 Newer approaches to treating hyperlipidemia include ezetimibe and fixed-dose combination therapy. The newer drug for treating high blood cholesterol levels is ezetimibe (Zetia).

Core Concept 16.9 Ezetimibe acts on the small intestine to block the absorption of dietary cholesterol. LDL-cholesterol and triglyceride levels are reduced, with a slight increase in HDL cholesterol.

New Approaches Ezetimibe (Zetia). Acts on the small intestine to block the absorption of dietary cholesterol. LDL-cholesterol and triglyceride levels are reduced, slight increase in HDL cholesterol. Combine drugs from two different classes in a single tablet. Combine an antihypertensive agent with an antihyperlipidemic drug.