Chapter 27 Antilipemic Drugs Copyright © 2014 by Mosby, an imprint of Elsevier Inc.

Chapter 27

Antilipemic Drugs

Copyright © 2014 by Mosby, an imprint of Elsevier Inc.

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

Triglycerides and Cholesterol

Copyright © 2014 by Mosby, an imprint of Elsevier Inc. 2

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”

Lipoproteins



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.

Cholesterol and Coronary Heart Disease (CHD)


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 (phenotyping)

Hyperlipidemias and Treatment Guidelines


All reasonable nondrug 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

Hyperlipidemias Treatment and Guidelines (cont’d)


HMG-CoA reductase inhibitors (HMGs, or statins)

Bile acid sequestrants B vitamin niacin (vitamin B3, nicotinic acid) Fibric acid derivatives (fibrates) Cholesterol absorption inhibitor (Zetia) Combination drugs (Vytorin)

Antilipemics


Most potent LDL reducers pravastatin (Pravachol) simvastatin (Zocor) atorvastatin (Lipitor) fluvastatin (Lescol) rosuvastatin (Crestor) pitavastatin (Livalo)

Antilipemics: HMG-CoA Reductase Inhibitors

(HMGs, or statins)


Inhibit HMG-CoA reductase, which is used by the liver to produce cholesterol

Lower the rate of cholesterol production

HMG-CoA Reductase Inhibitors: Mechanism of Action


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%

HMG-CoA Reductase Inhibitors: Indications


Mild, transient GI disturbances Rash Headache Myopathy (muscle pain), possibly leading to the

serious condition rhabdomyolysis Elevations in liver enzymes or liver disease

HMG-CoA Reductase Inhibitors: Adverse Effects


Oral anticoagulants Drugs metabolized by CYP3A4

erythromycin Azole antifungals verapamil diltiazem HIV protease inhibitors amiodarone Grapefruit juice

HMG-CoA Reductase Inhibitors: Interactions


Classroom Response Question

A patient with a new prescription for a HMG-CoA (statin) drug is instructed to take the medication with the evening meal or at bedtime. The patient asks why it must be taken at this time of day. The reason is:A.The medication is better absorbed at this time.

B.This timeframe correlates better with the natural diurnal rhythm of cholesterol production.

C.There will be fewer adverse effects if taken at night instead of with the morning meal.

D.This timing reduces the incidence of myopathy.


cholestyramine (Questran) colestipol (Colestid) colesevelam (Welchol) Also called bile acid–binding resins and

ion-exchange resins

Bile Acid Sequestrants


Prevent resorption of bile acids from small intestine

Bile acids are necessary for absorption of cholesterol

Bile Acid Sequestrants: Mechanism of Action


Type II hyperlipoproteinemia Relief of pruritus associated with partial biliary

obstruction (cholestyramine) May be used along with statins

Bile Acid Sequestrants: Indications


Constipation Heartburn, nausea, belching, bloating

These adverse effects tend to disappear over time

Bile Acid Sequestrants: Adverse Effects


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)


Thought to increase activity of lipase, which breaks down lipids

Reduces the metabolism or catabolism of cholesterol and triglycerides

Niacin: Mechanism of Action


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: Indications


Flushing (caused by histamine release) Pruritus GI distress

Niacin: Adverse Effects



A patient will be taking niacin as part of antilipemic therapy. The best way to avoid problems with flushing or pruritus would be to:

A.take the medication at bedtime.

B.take the medication with a small dose of a steroid.

C.take the medication with a full glass of water on an empty stomach.

D.start with a low initial dose, and then increase it gradually.


Also known as fibrates gemfibrozil (Lopid) fenofibrate (Tricor)

Fibric Acid Derivatives


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

Fibric Acid Derivatives: Mechanism of Action


Treatment of types III, IV, and V hyperlipidemias The fibric acid derivatives gemfibrozil and

fenofibrate decrease the triglyceride level and increase the HDL cholesterol level by as much as 25%

Fibric Acid Derivatives: Indications


Abdominal discomfort, diarrhea, nausea Blurred vision, headache Increased risk of gallstones Prolonged prothrombin time Liver studies may show increased enzyme levels

Fibric Acid Derivatives: Adverse Effects


Oral anticoagulants Statins

Risk for myositis, myalgias, and rhabdomyolysis is increased

Laboratory test reactions Decreased hemoglobin level, hematocrit value, and

white blood cell count Increased activated clotting time, lactate

dehydrogenase level, and bilirubin level

Fibric Acid Derivatives: Interactions


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 trials continue

• Currently recommended only when patients have not responded to other therapy

Cholesterol Absorption Inhibitor


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

Herbal Product: Garlic



A patient wants to take garlic tablets to improve his cholesterol levels. Which condition would be a contraindication?

A. Hypertension

B. Bowel obstruction

C. Sinus infection

D. Scheduled surgery


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

Herbal Product: Flax


Fish oil products Used to reduce cholesterol May cause rash, belching, allergic reactions Potential interactions with anticoagulant drugs

Herbal Product: Omega-3Fatty Acids


Before beginning therapy, obtain a thorough health and medication history

Assess dietary patterns, exercise level, weight, height, vital signs, tobacco and alcohol use, family history

Assess for contraindications, conditions that require cautious use, and drug interactions

Nursing Implications



Which patient would benefit from administration of simvastatin (Zocor) 80 mg? A.A patient newly diagnosed with hyperlipidemia

B.A patient with muscle aches who was taking another antilipidemic drug

C.A patient who is taking verapamil

D.A patient who has already been taking simvastatin (Zocor) for 12 months with no evidence of myopathy


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) Refer to guidelines regarding administration

times and meals

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



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



Before administering niacin, it is most important for the nurse to assess the patient for

A.allergy to erythromycin.

B.gout.

C.coronary artery disease.

D.hypothyroidism.



Small doses of aspirin or NSAIDs may be taken 30 minutes before niacin to minimize cutaneous flushing

Provide teaching regarding use of NSAIDs and aspirin

Inform patients that these drugs may take several weeks to show effectiveness



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



Date post:	19-Dec-2015
Category:	Documents
Upload:	emory-blake
View:	220 times
Download:	3 times

Chapter 27 Antilipemic Drugs Copyright © 2014 by Mosby, an imprint of Elsevier Inc.

Documents