1. Cardiovascular System
Antilipemics
Lilley, reading & workbook: Chap 28

2. Drugs used to lower lipid levels
Antilipemics
Drugs used to lower lipid levels

3. 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 a polipoprotein

4. 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”

6. Coronary Heart Disease
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

7. Coronary Heart Disease Positive Risk Factors
Age
Male 45 years or older
Female 55 years or older, or women with premature menopause not on estrogen replacement therapy
Family history: history of premature CHD
Current cigarette smoker
Hypertension
BP 140/90 or higher, or on antihypertensive medication
Low HDL levels: less than 35 mg/dL
Diabetes mellitus

8. Treatment Guidelines
Antilipemic drugs are used as an adjunct to diet therapy
Drug choice based on the specific lipid profile of the patient
All reasonable non-drug 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

9. Antilipemics HMG-CoA reductase inhibitors (HMGs, or statins)
Bile acid sequestrants
Niacin (nicotinic acid)
Fibric acid derivatives
Cholesterol absorption inhibitor
Combination drugs

10. Antilipemics: HMG-CoA Reductase Inhibitors (HMGs, or statins)
Most potent LDL reducers
lovastatin (Mevacor)
pravastatin (Pravachol)
simvastatin (Zocor)
atorvastatin (Lipitor)
fluvastatin (Lescol)

11. HMG-CoA Reductase Inhibitors (statins)
Indications
First-line drug therapy for hypercholesterolemia
Treatment of types IIa and IIb hyperlipidemias
Reduce LDL levels by 30% to 40%
Increase HDL levels by 2% to 15%
Reduce triglycerides by 10% to 30%

12. HMG-CoA Reductase Inhibitors (statins)
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

13. Bile Acid Sequestrants
cholestyramine (Questran)
colestipol hydrochloride (Colestid)
colesevelam (tablet form)
Also called bile acid–binding resins and ion-exchange resins

14. Bile Acid Sequestrants
Mechanism of action
Prevent resorption of bile acids from small intestine
Bile acids are necessary for absorption of cholesterol
Indications
Type II hyperlipoproteinemia
Relief of pruritus associated with partial biliary obstruction (cholestyramine)
May be used along with statins

15. Bile Acid Sequestrants
Adverse effects
Constipation
Heartburn, nausea, belching, bloating
These adverse effects tend to disappear over time

16. 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

17. Niacin (Nicotinic Acid)
Mechanism of action
Increases activity of lipase, which breaks down lipids
Reduces the metabolism of cholesterol and triglycerides
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

18. Niacin (Nicotinic Acid)
Adverse effects
Flushing (due to histamine release)
Pruritus
GI distress

19. Fibric Acid Derivatives
Also known as fibrates
gemfibrozil (Lopid)
fenofibrate (Tricor)

20. Fibric Acid Derivatives
Mechanism of action
Activate lipase, which breaks down cholesterol
Suppress release of free fatty acid from the adipose tissue, inhibit synthesis of triglycerides in the liver, and increase the secretion of cholesterol in the bile
Indications
Treatment of types III, IV, and V hyperlipidemias
Drug Effects
Decrease the triglyceride levels
Increase HDL by as much as 25%

21. Fibric Acid Derivatives
Adverse effects
Abdominal discomfort, diarrhea, nausea
Blurred vision, headache
Increased risk of gallstones
Prolonged prothrombin time
Liver studies may show increased function

22. Cholesterol Absorption Inhibitor
ezetimibe (Zetia)
Inhibits absorption of cholesterol and related sterols from the small intestine
Results in reduced total cholesterol, LDL, triglylceride levels
Also increases HDL levels
Works well when taken with a statin drug

23. Nursing Implications Patient Education
Before beginning therapy, obtain a thorough health and medication history
Assess dietary patterns, exercise level, weight, height, VS, tobacco and alcohol use, family history
Assess for contraindications, conditions that require cautious use, and drug interactions

24. Nursing Implications Patient Education
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)
Take with meals to decrease GI upset

25. Nursing Implications Patient Education
Patient must be counseled concerning diet and nutrition on an ongoing basis
Instruct on proper procedure for taking the medications
Powder forms must be taken with a liquid, mixed thoroughly but not stirred, and NEVER taken dry

26. Nursing Implications Patient Education
Other medications should be taken 1 hour before or 4 to 6 hours after meals to avoid interference with absorption
Clofibrate often causes constipation; instruct patients to increase fiber and fluid intake to offset this effect

27. Nursing Implications Patient Education
To minimize adverse effects of niacin, start on low initial dose and gradually increase it, and take with meals
Small doses of aspirin or NSAIDs may be taken 30 minutes before niacin to minimize cutaneous flushing
Inform patients that these drugs may take several weeks to show effectiveness

28. Nursing Implications Patient Education
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

29. Review
In addition to drug therapy, the patient should be encouraged to do which of the following to treat hyperlipidemia? (Select all that apply.)
1. Reduce cholesterol and fats in diet.
2. Reduce weight.
3. Decrease exercise.
4. Increase use of polyunsaturated and
monounsaturated fats.

30. Review
Before initiating a statin drug, the premedication assessment should include: 1. complete blood count (CBC). 2. liver function studies. 3. bleeding time. 4. gastrointestinal (GI) series.

31. Review
Ezetimibe (Zetia) acts by: 1. an unknown mechanism of action. 2. binding bile acids in the intestines. 3. removing fat-soluble vitamins. 4. blocking absorption of cholesterol by the small intestines.