Chap 27 Antilipemic Drugs

Question 1

Triglycerides and Cholesterol***

Answer 1

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.

Question 1

Lipoproteins

Answer 1

Very-low-density lipoprotein (VLDL)**
Produced by the liver
Transports endogenous lipids to the cells
Low-density lipoprotein (LDL)**
BAD CHOLESTEROL LOWER THE BETTER
Optimal: <100 mg/dL
very high: 190 mg/dL
High-density lipoprotein (HDL)**
GOOD CHOLESTEROL HIGHER THE BETTER
<40 mg/dL major risk for heart disease
Responsible for “recycling” of cholesterol
Also known as “good cholesterol”

TOTAL CHOLESTEROL
BEST:200 mg/dL or below
Borderline: 200-239
High: 240 or above

Question 2

ARTERIOSCLEROSIS**

Answer 2

[ARTERIO] - Artery
[SCLEROSIS] - Hardening
Definition - hardening from plaque “ atheromatous plaque”

Question 3

Hyperlipidemias and Treatment Guidelines

Answer 3

National Cholesterol Education Program Adult Treatment Panel III of the National Institutes of Health
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)

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.

Question 4

Antilipemics

Answer 4

ACC/AHA Guideline on the Treatment of Blood Cholesterol to Reduce Atherosclerotic Cardiovascular Risk in Adults (2013)
Hydroxymethylglutaryl–coenzyme A (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)**

Question 5

Newer Agents

Answer 5

Mipomersen:* once-weekly subcutaneous injection*
Microsomal triglyceride transfer protein inhibitor
Lomitapide (Juxtapid)**
Proprotein convertase subtilisin kexin 9 *(PCSK9) *inhibitors
Alirocumab (Praluent)**
Evolocumab (Repatha)**

Question 6

Antilipemics: HMG-CoA Reductase Inhibitors (Statins)**

Answer 6

Statins**
Patients with clinical atherosclerotic cardiovascular disease (CVD)
Patients with LDL cholesterol levels >190 mg/dL
Patients with diabetes* age 40 to 75 years with LDL levels of 70 to 189 mg/dL and* without evidence of CVD*
Patients without evidence of CVD or diabetes but who have LDL levels between 70 and 189 mg/dL and a 10-year risk of CVD > 7.5%

Question 7

Antilipemics: HMG-CoA Reductase Inhibitors (Statins)

Answer 7

Most potent LDL reducers
Lovastatin* (Mevacor)
Pravastatin (Pravachol)
Simvastatin (Zocor)
Atorvastatin (Lipitor)
Fluvastatin (Lescol)
Rosuvastatin (Crestor)
Pitavastatin (Livalo)

Question 8

HMG-CoA Reductase Inhibitors: Mechanism of Action*

Answer 8

Inhibit HMG-CoA reductase, which is used by the liver to produce cholesterol
Lower the rate of cholesterol production

Question 9

HMG-CoA Reductase Inhibitors: Indications

Answer 9

First-line drug therapy for hypercholesterolemia
Treatment of types IIa and IIb hyperlipidemias
Reduces LDL levels by up to 50%
Increases HDL levels by 2% to 15%
Reduces triglycerides by 10% to 30%

Question 10

HMG-CoA Reductase Inhibitors: Adverse* Effects

Answer 10

Mild, transient gastrointestinal (GI) disturbances
Rash
Headache*
Myopathy (muscle pain), possibly leading to the serious condition rhabdomyolysis
Elevations in liver enzymes or liver disease

Question 10

Rhabdomyloysis

Answer 10

Breakdown of muscle protein
Myoglobinuria: urinary elimination of the muscle protein myoglobin
Can lead to acute renal failure and even death
When recognized reasonably early, rhabdomyolysis is usually reversible with discontinuation of the statin drug.
Instruct patients to immediately report any signs of toxicity, including muscle soreness or changes in urine color.

Question 11

HMG-CoA Reductase Inhibitors: Interactions*

Answer 11

Oral anticoagulants*
Drugs metabolized by Cytochrome P-450*
Erythromycin
Azole antifungals**
Verapamil
Diltiazem
Human immunodeficiency virus protease inhibitors
Amiodarone**
Grapefruit juice**

Question 12

Atorvastatin (Lipitor) **

Answer 12

One of the most commonly used drugs in this class of cholesterol-lowering drugs
Lowers total and LDL cholesterol levels as well as triglyceride levels and raises “good” cholesterol, the HDL component
Dosed once daily**, usually with the evening meal or at bedtime to correlate with diurnal rhythm

Question 12

Simvastatin (Zocor)**

Answer 12

One of the first statins to become generic and one of the most commonly used drugs in this class
Used to primarily lower total and LDL cholesterol levels as well as triglyceride levels
Can moderately raise levels of HDL
Many drug interactions which may require dosing adjustments

Question 13

Bile Acid Sequestrants **

Answer 13

Cholestyramine (Questran)**
Colestipol (Colestid)**
Tablet form
Colesevelam (Welchol)**
Also called bile acid–binding resins and 
ion-exchange resins
Powdered form may not be convenient or well tolerated

Question 14

Bile Acid Sequestrants: 
Mechanism of Action

Answer 14

Considered second line choice after statins
Prevent resorption of bile acids from small intestine**
Bile acids are necessary for absorption 
of cholesterol.

Question 15

Bile Acid Sequestrants: 
Adverse Effects

Answer 15

Constipation**
Heartburn, nausea, belching, bloating
These adverse effects tend to disappear over time.
Increasing dietary fiber intake or taking a fiber supplement such as psyllium (Metamucil and others), as well as increasing fluid intake, may relieve constipation and bloating.
May also cause mild increases in triglyceride levels

Question 16

Bile Acid Sequestrants: 
Considerations

Answer 16

Overdose can cause obstruction because the bile acid sequestrants are not absorbed.
Treatment of overdose includes restoring gut motility.
Drug interactions**
All drugs must be taken at least 1 hour before or 4 to 6 hours after the administration of bile acid sequestrants.
High doses of a bile acid sequestrant decrease the absorption of fat-soluble vitamins (A, D, E, and K).

Question 17

Niacin *(Nicotinic Acid)

Answer 17

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

Question 18

Niacin: Mechanism of Action

Answer 18

Thought to increase activity of lipase, which breaks down lipids
Reduces the metabolism or catabolism of cholesterol and triglycerides

Question 19

Niacin: Indications

Answer 19

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

Question 20

Niacin: Adverse Effects**

Answer 20

Flushing (caused by histamine release)**
Small dose aspirin or NSAIDS 30 minutes before Niacin may help cutaneous flushing**
Pruritus
GI distress

Question 21

Fibrates**

Answer 21

Group of lipid-lowering meds along w/ statins and niacin

*Effective at lowering triglyceride levels**

less effective at controlling cholesterol

Question 22

Fibric Acid Derivatives

Answer 22

Primarily affect the triglyceride levels but may also lower the total cholesterol and LDL levels and raise the HDL
Also known as fibrates
Gemfibrozil (Lopid)**
Fenofibrate (Tricor)**

Question 23

Fibric Acid Derivatives:
Mechanism of Action

Answer 23

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

Question 23

Fibric Acid Derivatives: Contraindications**

Answer 23

Known drug allergy**
Severe liver or kidney disease**
Cirrhosis**
Gallbladder disease**

Question 24

Fibric Acid Derivatives: 
Adverse Effects**

Answer 24

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

Question 25

Fibric Acid Derivatives: 
Interactions*

Answer 25

Oral anticoagulants
Statins*
Risk of 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

Question 26

Miscellaneous Antilipemic Drugs:
Cholesterol Absorption Inhibitor

Answer 26

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
Can be used as monotherapy

Question 27

Alirocumab (Praluent)**

Answer 27

Approved in 2015
Given subcutaneously every 2 to 4 weeks
Very expensive
Adverse effects: diarrhea, increased liver function tests, influenza, hypersensitivity reactions, injection site reaction, myalgia, cough

Question 28

Herbal Product: Garlic *

Answer 28

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 nonsteroidal antiinflammatory drugs (NSAIDs)*

Question 29

Herbal Product: Flax*

Answer 29

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

Question 30

Herbal Product: Omega-3
Fatty Acids

Answer 30

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

Question 31

Nursing Implications**

Answer 31

Before beginning therapy, obtain a thorough health and medication history.
*Assess dietary patterns, exercise level, weight, height, vital signs, tobacco and alcohol use, and family history.**
Assess for contraindications**, conditions that require cautious use, and drug interactions.

Contraindications* include biliary obstruction, liver dysfunction, and active liver disease.**
Obtain baseline liver function studies.
Patients on long-term therapy** may need *supplemental fat-soluble vitamins (A, D, E, K).
Refer to guidelines regarding administration times and meals.

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 with food or fluids (4-6 oz of fluid)**
Never take the powder 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.**

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 (6-8 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