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7/29/2019 12 Antilipemics Upd
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Copyright 2002, 1998, Elsevier Science (USA). All rights reserved.
Antilipemic Agents
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Copyright 2002, 1998, Elsevier Science (USA). All rights reserved.
Antilipemics
Drugs used to lower lipid levels
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Copyright 2002, 1998, Elsevier Science (USA). All rights reserved.
Triglycerides and Cholesterol
Two primary forms of lipids in the blood
Water-insoluble fats that must be bound to
apoproteins, specialized lipid-carryingproteins
Lipoprotein is the the combination of
triglyceride or cholesterol with apoprotein
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Copyright 2002, 1998, Elsevier Science (USA). All rights reserved.
Types of Lipoproteins
Lipid ProteinContent Lipoprotein Classification Content
Most chylomicron Least
very-low density lipoprotein(VLDL)
Intermediate-density lipoprotein(IDL)
Least High-density lipoprotein (HDL) Most
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Copyright 2002, 1998, Elsevier Science (USA). All rights reserved.
Instructors may want to insert
EIC Image #84:
Cholesterol Homeostasis
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Copyright 2002, 1998, Elsevier Science (USA). All rights reserved.
Coronary Heart Disease
The risk of CHD in patients with cholesterollevels of 300 mg/dL is 3 to 4 times greaterthan that in patients with levels less than300 mg/dL
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Copyright 2002, 1998, Elsevier Science (USA). All rights reserved.
Antilipemics
Bile acid sequestrants
HMG-CoA reductase inhibitors
(HMGs or statins)
Fibric acid derivatives
Niacin (nicotinic acid)
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Copyright 2002, 1998, Elsevier Science (USA). All rights reserved.
Antilipemics: Bile Acid Sequestrants
cholestyramine (Questran)
colestipol hydrochloride (Colestid)
Also called bile acid-binding resins andion-exchange resins
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Copyright 2002, 1998, Elsevier Science (USA). All rights reserved.
Antilipemics: Bile Acid Sequestrants
Mechanism of Action
Prevent resorption of bile acids from small intestine
Bile acids are necessary for absorptionof cholesterol
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Copyright 2002, 1998, Elsevier Science (USA). All rights reserved.
Antilipemics: Bile Acid Sequestrants
Therapeutic Uses
Type II hyperlipoproteinemia
Relief of pruritus associated with partial biliaryobstruction (cholestyramine)
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Copyright 2002, 1998, Elsevier Science (USA). All rights reserved.
Antilipemics: Bile Acid Sequestrants
Side Effects
Constipation
Heartburn, nausea, belching, bloating
These adverse effects tend to disappear over time
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Copyright 2002, 1998, Elsevier Science (USA). All rights reserved.
Antilipemics: HMG-CoA Reductase
Inhibitors (HMGs or statins) lovastatin (Mevacor)
pravastatin (Pravachol)
simvastatin (Zocor)
atorvastatin (Lipitor)
cerivastatin (Baycol)
fluvastatin (Lescol)
Most potent LDL reducers
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Copyright 2002, 1998, Elsevier Science (USA). All rights reserved.
Antilipemics:
HMG-CoA Reductase InhibitorsMechanism 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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Copyright 2002, 1998, Elsevier Science (USA). All rights reserved.
Antilipemics:
HMG-CoA Reductase InhibitorsTherapeutic Uses
Treatment of type 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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Copyright 2002, 1998, Elsevier Science (USA). All rights reserved.
Antilipemics:
HMG-CoA Reductase InhibitorsSide Effects
Mild, transient GI disturbances
Rash
Headache
Myopathy (muscle pain)
Elevations in liver enzymes
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Copyright 2002, 1998, Elsevier Science (USA). All rights reserved.
Antilipemics: Fibric Acid Derivatives
clofibrate
gemfibrozil (Lopid)
fenofibrate (Tricor)
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Copyright 2002, 1998, Elsevier Science (USA). All rights reserved.
Antilipemics: Fibric Acid Derivatives
Mechanism of Action
Believed to work by activating lipase, which
breaks down cholesterol
Also suppress release of free fatty acid fromthe adipose tissue, inhibit synthesis oftriglycerides in the liver, and increase thesecretion of cholesterol in the bile
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Copyright 2002, 1998, Elsevier Science (USA). All rights reserved.
Antilipemics: Fibric Acid Derivatives
Therapeutic Uses
Treatment of type IV and V hyperlipemias
Treatment of type III, IV, and Vhyperlipidemias
Decrease the triglyceride levels and increaseHDL by as much as 25%
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Copyright 2002, 1998, Elsevier Science (USA). All rights reserved.
Antilipemics: Fibric Acid Derivatives
Side Effects
Abdominal discomfort
Diarrhea Nausea
Blurred vision
Increased risk of gallstones
Prolonged prothrombin time
Liver studies may show increased function
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Copyright 2002, 1998, Elsevier Science (USA). All rights reserved.
Antilipemics: Niacin (Nicotinic Acid)
Vitamin B3
Lipid-lowering properties require much
higher doses than when used as a vitamin
Effective, inexpensive, often used incombination with other lipid-lowering agents
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Copyright 2002, 1998, Elsevier Science (USA). All rights reserved.
Antilipemics: Niacin (Nicotinic Acid)
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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Copyright 2002, 1998, Elsevier Science (USA). All rights reserved.
Antilipemics: Niacin (Nicotinic Acid)
Therapeutic Uses
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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Copyright 2002, 1998, Elsevier Science (USA). All rights reserved.
Antilipemics: Niacin (Nicotinic Acid)
Side Effects
Flushing (due to histamine release)
Pruritus
GI distress
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Copyright 2002, 1998, Elsevier Science (USA). All rights reserved.
Antilipemics: Nursing Implications
Before beginning therapy, obtain a thoroughhealth and medication history.
Assess dietary patterns, exercise level,weight, height, VS, tobacco and alcoholuse, family history.
Assess for contraindications, conditions thatrequire cautious use, and drug interactions.
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Copyright 2002, 1998, Elsevier Science (USA). All rights reserved.
Antilipemics: Nursing Implications
Contraindications include biliary obstruction,liver dysfunction, active liver disease.
Obtain baseline liver function studies.
Patients on long-term therapy may needsupplemental fat-soluble vitamins (A, D, K).
Take with meals to decrease GI upset.
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Copyright 2002, 1998, Elsevier Science (USA). All rights reserved.
Antilipemics: Nursing Implications
Patient must be counseled concerning diet andnutrition on an ongoing basis.
Instruct on proper procedure for taking themedications.
Powder forms must be taken with a liquid, mixedthoroughly but not stirred, and NEVER taken dry.
Other medications should be taken 1 hour beforeor 4 to 6 hours after meals to avoid interferencewith absorption.
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Copyright 2002, 1998, Elsevier Science (USA). All rights reserved.
Antilipemics: Nursing Implications
Clofibrate often causes constipation; instructpatients to increase fiber and fluid intake tooffset this effect.
To minimize side effects of niacin, start onlow initial dose and gradually increase it,and take with meals.
Small doses of aspirin or NSAIDs may betaken 30 minutes before niacin to minimizecutaneous flushing.
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Copyright 2002, 1998, Elsevier Science (USA). All rights reserved.
Antilipemics: Nursing Implications
Inform patients that these agents may takeseveral weeks to show effectiveness.
Instruct patients to report persistent GIupset, constipation, abnormal or unusualbleeding, and yellow discoloration of theskin.
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Copyright 2002, 1998, Elsevier Science (USA). All rights reserved.
Antilipemics: Nursing Implications
Monitor for side effects, including increasedliver enzyme studies.
Monitor for therapeutic effects: Reduced cholesterol and triglyceride levels