Antilipemics

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Cardiovascular System

• Antilipemics
• Lilley, reading workbook Chap 28

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Antilipemics

• Drugs used to lower lipid levels

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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 a polipoprotein

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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 DiseasePositive 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

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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

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Antilipemics

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

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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 (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

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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

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Bile Acid Sequestrants

• cholestyramine (Questran)
• colestipol hydrochloride (Colestid)
• colesevelam (tablet form)
• Also called bile acidbinding 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
• 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 (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

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Niacin (Nicotinic Acid)

• Adverse effects
• Flushing (due to 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
• 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

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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,
  triglylceride levels
• Also increases HDL levels
• Works well when taken with a statin drug

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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

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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

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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

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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

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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

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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

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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.
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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.

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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.