Cardiovascular System

ANTILIPEMICS

LILLEY, READING & WORKBOOK: CHAP 28

 Antilipemics

Drugs used to lower lipid levels

 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
 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”
 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
 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
 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
 Antilipemics

HMG-CoA reductase inhibitors

(HMGs, or statins)
Bile acid sequestrants
Niacin (nicotinic acid)
Fibric acid derivatives
Cholesterol absorption inhibitor
Combination drugs
Antilipemics: HMG-CoA Reductase
Inhibitors (HMGs, or statins)

Most potent LDL reducers

lovastatin (Mevacor)
pravastatin (Pravachol)
simvastatin (Zocor)
atorvastatin (Lipitor)
fluvastatin (Lescol)
 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%

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
 Bile Acid Sequestrants

cholestyramine (Questran)

colestipol hydrochloride (Colestid)

colesevelam (tablet form)

Also called bile acid–binding resins and

ion-exchange resins
 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
 Bile Acid Sequestrants

Adverse effects

 Constipation

 Heartburn, nausea, belching, bloating

 These adverse effects tend to disappear over
time
 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
 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
 Niacin (Nicotinic Acid)

Adverse effects

 Flushing (due to histamine release)

 Pruritus
 GI distress
 Fibric Acid Derivatives

Also known as fibrates

gemfibrozil (Lopid)
fenofibrate (Tricor)
 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%
 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
 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
 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
 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

 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
 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
 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
 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
 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.
 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.
 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.