1. Copyright © 2014 by Mosby, an imprint of Elsevier Inc.
Chapter 27
Antilipemic Drugs
Copyright © 2014 by Mosby, an imprint of Elsevier Inc.

2. Triglycerides and Cholesterol
Two primary forms of lipids in the blood
Water-insoluble fats that must be bound to apolipoproteins, specialized lipid-carrying proteins
Lipoprotein is the combination of triglyceride or cholesterol with apolipoprotein
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3. Copyright © 2014 by Mosby, an imprint of Elsevier Inc.
Lipoproteins
Very-low-density lipoprotein (VLDL)
Produced by the liver
Transports endogenous lipids to the cells
Low-density lipoprotein (LDL)
High-density lipoprotein (HDL)
Responsible for “recycling” of cholesterol
Also known as “good cholesterol”
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5. Cholesterol and Coronary Heart Disease (CHD)
The risk of CHD in patients with cholesterol levels of 300 mg/dL is three to four times greater than that in patients with levels less than 200 mg/dL.
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6. Hyperlipidemias and Treatment Guidelines
Antilipemic drugs
Drugs used to lower lipid levels
Used as an adjunct to diet therapy
Drug choice based on the specific lipid profile of the patient (phenotyping)
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7. Hyperlipidemias Treatment and Guidelines (cont’d)
All reasonable nondrug means of controlling blood cholesterol levels (e.g., diet, exercise) should be tried for at least 6 months and found to fail before drug therapy is considered
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8. Copyright © 2014 by Mosby, an imprint of Elsevier Inc.
Antilipemics
HMG-CoA reductase inhibitors (HMGs, or statins)
Bile acid sequestrants
B vitamin niacin (vitamin B3, nicotinic acid)
Fibric acid derivatives (fibrates)
Cholesterol absorption inhibitor (Zetia)
Combination drugs (Vytorin)
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9. Antilipemics: HMG-CoA Reductase Inhibitors (HMGs, or statins)
Most potent LDL reducers
pravastatin (Pravachol)
simvastatin (Zocor)
atorvastatin (Lipitor)
fluvastatin (Lescol)
rosuvastatin (Crestor)
pitavastatin (Livalo)
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10. HMG-CoA Reductase Inhibitors: Mechanism of Action
Inhibit HMG-CoA reductase, which is used by the liver to produce cholesterol
Lower the rate of cholesterol production
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11. HMG-CoA Reductase Inhibitors: Indications
First-line drug therapy for hypercholesterolemia
Treatment of types IIa and IIb hyperlipidemias
Reduces LDL levels by 30% to 40%
Increases HDL levels by 2% to 15%
Reduces triglycerides by 10% to 30%
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12. HMG-CoA Reductase Inhibitors: Adverse Effects
Mild, transient GI disturbances
Rash
Headache
Myopathy (muscle pain), possibly leading to the serious condition rhabdomyolysis
Elevations in liver enzymes or liver disease
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13. HMG-CoA Reductase Inhibitors: Interactions
Oral anticoagulants
Drugs metabolized by CYP3A4
erythromycin
Azole antifungals
verapamil
diltiazem
HIV protease inhibitors
amiodarone
Grapefruit juice
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14. Classroom Response Question
A patient with a new prescription for a HMG-CoA (statin) drug is instructed to take the medication with the evening meal or at bedtime. The patient asks why it must be taken at this time of day. The reason is:
The medication is better absorbed at this time.
This timeframe correlates better with the natural diurnal rhythm of cholesterol production.
There will be fewer adverse effects if taken at night instead of with the morning meal.
This timing reduces the incidence of myopathy.
Correct answer: B
Rationale: All statins are generally dosed once daily, usually with the evening meal or at bedtime, to better coincide with the body’s natural diurnal rhythm of cholesterol production.
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15. Bile Acid Sequestrants
cholestyramine (Questran)
colestipol (Colestid)
colesevelam (Welchol)
Also called bile acid–binding resins and ion-exchange resins
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16. Bile Acid Sequestrants: Mechanism of Action
Prevent resorption of bile acids from small intestine
Bile acids are necessary for absorption of cholesterol
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17. Bile Acid Sequestrants: Indications
Type II hyperlipoproteinemia
Relief of pruritus associated with partial biliary obstruction (cholestyramine)
May be used along with statins
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18. Bile Acid Sequestrants: Adverse Effects
Constipation
Heartburn, nausea, belching, bloating
These adverse effects tend to disappear over time
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19. Niacin (Nicotinic Acid)
Vitamin B3
Lipid-lowering properties require much higher doses than when used as a vitamin
Effective, inexpensive, often used in combination with other lipid-lowering drugs
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20. Niacin: Mechanism of Action
Thought to increase activity of lipase, which breaks down lipids
Reduces the metabolism or catabolism of cholesterol and triglycerides
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21. Copyright © 2014 by Mosby, an imprint of Elsevier Inc.
Niacin: Indications
Effective in lowering triglyceride, total serum cholesterol, and LDL levels
Increases HDL levels
Effective in the treatment of types IIa, IIb, III, IV, and V hyperlipidemias
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22. Niacin: Adverse Effects
Flushing (caused by histamine release)
Pruritus
GI distress
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23. Classroom Response Question
A patient will be taking niacin as part of antilipemic therapy. The best way to avoid problems with flushing or pruritus would be to:
take the medication at bedtime.
take the medication with a small dose of a steroid.
take the medication with a full glass of water on an empty stomach.
start with a low initial dose, and then increase it gradually.
Correct answer: D
Rationale: Cutaneous flushing may be minimized if the niacin is started at a smaller dose and gradually increased. Premedication with a small dose of aspirin or a nonsteroidal antiinflammatory drug (NSAID) 30 minutes before taking the niacin, as well as taking the niacin with meals, may help to minimize these undesirable effects.
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24. Fibric Acid Derivatives
Also known as fibrates
gemfibrozil (Lopid)
fenofibrate (Tricor)
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25. Fibric Acid Derivatives: Mechanism of Action
Believed to work by activating lipase, which breaks down cholesterol
Also suppress the release of free fatty acid from adipose tissue, inhibit synthesis of triglycerides in the liver, and increase secretion of cholesterol in the bile
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26. Fibric Acid Derivatives: Indications
Treatment of types III, IV, and V hyperlipidemias
The fibric acid derivatives gemfibrozil and fenofibrate decrease the triglyceride level and increase the HDL cholesterol level by as much as 25%
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27. Fibric Acid Derivatives: Adverse Effects
Abdominal discomfort, diarrhea, nausea
Blurred vision, headache
Increased risk of gallstones
Prolonged prothrombin time
Liver studies may show increased enzyme levels
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28. Fibric Acid Derivatives: Interactions
Oral anticoagulants
Statins
Risk for myositis, myalgias, and rhabdomyolysis is increased
Laboratory test reactions
Decreased hemoglobin level, hematocrit value, and white blood cell count
Increased activated clotting time, lactate dehydrogenase level, and bilirubin level
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29. Cholesterol Absorption Inhibitor
ezetimibe (Zetia)
Inhibits absorption of cholesterol and related sterols from the small intestine
Results in reduced total cholesterol, LDL, and triglyceride levels
Also increases HDL levels
Often combined with a statin drug
Clinical trials continue
Currently recommended only when patients have not responded to other therapy
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30. Herbal Product: Garlic
Used as an antispasmodic, antihypertensive, antiplatelet, lipid reducer
Adverse effects: dermatitis, vomiting, diarrhea, flatulence, antiplatelet activity
Possible interactions with warfarin, diazepam
May enhance bleeding when taken with NSAIDs
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31. Classroom Response Question
A patient wants to take garlic tablets to improve his cholesterol levels. Which condition would be a contraindication?
Hypertension
Bowel obstruction
Sinus infection
Scheduled surgery
Correct answer: D
Rationale: Garlic has antiplatelet activity, and is contraindicated in patients who will undergo surgery within 2 weeks and in patients with human immunodeficiency virus infection or diabetes.
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Herbal Product: Flax
Both the seed and oil of the plant are used
Uses: atherosclerosis, hypercholesterolemia, GI distress, menopausal symptoms
May cause diarrhea and allergic reactions
Possible interactions: antidiabetic drugs, anticoagulant drugs
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33. Herbal Product: Omega-3 Fatty Acids
Fish oil products
Used to reduce cholesterol
May cause rash, belching, allergic reactions
Potential interactions with anticoagulant drugs
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34. Copyright © 2014 by Mosby, an imprint of Elsevier Inc.
Nursing Implications
Before beginning therapy, obtain a thorough health and medication history
Assess dietary patterns, exercise level, weight, height, vital signs, tobacco and alcohol use, family history
Assess for contraindications, conditions that require cautious use, and drug interactions
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35. Classroom Response Question
Which patient would benefit from administration of simvastatin (Zocor) 80 mg?
A patient newly diagnosed with hyperlipidemia
A patient with muscle aches who was taking another antilipidemic drug
A patient who is taking verapamil
A patient who has already been taking simvastatin (Zocor) for 12 months with no evidence of myopathy
Correct answer D
Rationale: In 2011, the FDA imposed new prescribing restrictions on simvastatin, stating “Physicians should limit using the 80-mg dose unless the patient has already been taking the drug for 12 months and there is no evidence of myopathy. Simvastatin 80 mg should not be started in new patients, including patients already taking lower doses of the drug.” In patients taking verapamil, the dose of simvastatin is not to exceed 10 mg.
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36. Nursing Implications (cont’d)
Contraindications include biliary obstruction, liver dysfunction, active liver disease
Obtain baseline liver function studies
Patients on long-term therapy may need supplemental fat-soluble vitamins (A, D, K)
Refer to guidelines regarding administration times and meals
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37. Nursing Implications (cont’d)
Counsel patient concerning diet and nutrition on an ongoing basis
Instruct patient on proper procedure for taking the medications
Powder forms must be taken with a liquid, mixed thoroughly but not stirred, and never taken dry
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38. Nursing Implications (cont’d)
Other medications should be taken 1 hour before or 4 to 6 hours after meals to avoid interference with absorption
To minimize adverse effects of niacin, start on low initial dose and gradually increase it, and take with meals
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39. Classroom Response Question
Before administering niacin, it is most important for the nurse to assess the patient for
allergy to erythromycin.
gout.
coronary artery disease.
hypothyroidism.
Correct answer: B
Rationale: With niacin, patient assessment includes noting contraindications such as liver disease, peptic ulcer disease, gout, hypertension, and any active bleeding. Although a thorough assessment of all patient conditions is helpful, the other conditions do not preclude use of niacin.
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40. Nursing Implications (cont’d)
Small doses of aspirin or NSAIDs may be taken 30 minutes before niacin to minimize cutaneous flushing
Provide teaching regarding use of NSAIDs and aspirin
Inform patients that these drugs may take several weeks to show effectiveness
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41. Nursing Implications (cont’d)
Instruct patients to report persistent GI upset, constipation, abnormal or unusual bleeding, and yellow discoloration of the skin
Monitor for adverse effects, including increased liver enzyme studies
Monitor for therapeutic effects
Reduced cholesterol and triglyceride levels
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