CHAPTER 29
Antilipemic Drugs
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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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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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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
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Coronary Heart Disease
Positive Risk Factors

Age

Male 45 years or older
 Female 55 years or older
 Family history of premature CHD

Current cigarette smoker
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Coronary Heart Disease
Positive Risk Factors (cont’d)

Hypertension



BP 140/90 or higher, or on antihypertensive
medication
Low HDL levels: less than 40 mg/dL
Diabetes mellitus
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Coronary Heart Disease
Negative (Beneficial) Risk Factor

High HDL (“good” cholesterol): 60 mg/dL or
higher
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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
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Treatment Guidelines (cont’d)

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
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Antilipemics






HMG-CoA reductase inhibitors (HMGs, or
statins)
Bile acid sequestrants
Niacin (nicotinic acid)
Fibric acid derivatives (fibrates)
Cholesterol absorption inhibitor (Zetia)
Combination drugs (Vytorin)
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Antilipemics:
HMG-CoA Reductase Inhibitors
(HMGs, or statins)

Most potent LDL reducers

lovastatin (Mevacor)
 pravastatin (Pravachol)
 simvastatin (Zocor)
 atorvastatin (Lipitor)
 fluvastatin (Lescol)
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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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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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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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Bile Acid Sequestrants




cholestyramine (Questran)
colestipol hydrochloride (Colestid)
colesevelam (tablet form only)
Also called bile acid–binding resins and
ion-exchange resins
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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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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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Bile Acid Sequestrants:
Adverse Effects


Constipation
Heartburn, nausea, belching, bloating

These adverse effects tend to disappear over
time
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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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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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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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Niacin: Adverse Effects



Flushing (caused by histamine release)
Pruritus
GI distress
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Fibric Acid Derivatives

Also known as fibrates


gemfibrozil (Lopid)
fenofibrate (Tricor)
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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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Fibric Acid Derivatives:
Indications

Treatment of types III, IV, and V
hyperlipidemias
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Fibric Acid Derivatives:
Drug Effects


Decrease the triglyceride levels
Increase HDL by as much as 25%
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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
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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 usefulness has been questioned; new
trials underway
Currently recommended only when patients have not
responded to other therapy
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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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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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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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Nursing Implications



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
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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)
Take with meals to decrease GI upset
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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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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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Nursing Implications (cont’d)


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
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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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