12 antilipemics upd

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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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

apoproteins, specialized lipid-carryingproteins

Lipoprotein is the the combination of

triglyceride or cholesterol with apoprotein


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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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Instructors may want to insert

EIC Image #84:

Cholesterol Homeostasis


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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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Antilipemics

Bile acid sequestrants

HMG-CoA reductase inhibitors

(HMGs or statins)

Fibric acid derivatives

Niacin (nicotinic acid)


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Antilipemics: Bile Acid Sequestrants

cholestyramine (Questran)

colestipol hydrochloride (Colestid)

Also called bile acid-binding resins andion-exchange resins


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Mechanism of Action

Prevent resorption of bile acids from small intestine

Bile acids are necessary for absorptionof cholesterol


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Therapeutic Uses

Type II hyperlipoproteinemia

Relief of pruritus associated with partial biliaryobstruction (cholestyramine)


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Side Effects

Constipation

Heartburn, nausea, belching, bloating

These adverse effects tend to disappear over time


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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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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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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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Antilipemics:

HMG-CoA Reductase InhibitorsSide Effects

Mild, transient GI disturbances

Rash

Headache

Myopathy (muscle pain)

Elevations in liver enzymes


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Antilipemics: Fibric Acid Derivatives

clofibrate

gemfibrozil (Lopid)

fenofibrate (Tricor)


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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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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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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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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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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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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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Side Effects

Flushing (due to histamine release)

Pruritus

GI distress


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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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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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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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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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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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Monitor for side effects, including increasedliver enzyme studies.

Monitor for therapeutic effects: Reduced cholesterol and triglyceride levels

12 antilipemics upd

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