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STUDY CARDS > Antilipemic Drugs > Flashcards

Antilipemic Drugs Flashcards

1
Q

Two primary forms of lipids in the blood?

What are they used for?

Water-insoluble fats that must be bound to __________

A

Triglycerides and Cholesterol

Triglycerides (energy source stored in adipose)
Cholesterol (used to make steroid hormones, cell membranes, and bile acid)

Water-insoluble fats that must be bound to apolipoproteins, specialized lipid-carrying proteins

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2
Q

Apolipoproteins

A

specialized lipid-carrying proteins

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3
Q

Lipoprotein is the combination of?

A

Lipoprotein is the combination of triglyceride or cholesterol with apolipoprotein.

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4
Q

Lipoprotein

A

transport lipids via the blood

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5
Q

4 types of lipoprotein

A

Very-low-density lipoprotein

Intermediate-density lipoprotein

Low-density lipoprotein (LDL)

High-density lipoprotein (HDL)

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6
Q

Very-low-density lipoprotein

produced by?

transports? to?

A

Produced by the liver

Transports endogenous lipids to peripheral cells

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7
Q

Intermediate-density lipoprotein

A
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8
Q

Low-density lipoprotein (LDL)

A

bad cholesterol

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9
Q

High-density lipoprotein (HDL)

responsible for?

also known as?

produced in the?

formed when?

A

Responsible for “recycling” of cholesterol

Also known as “good cholesterol” (cardioprotective)

produced in the liver and intestines

formed when chylomicrons are broken down

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10
Q

Cholesterol and Coronary Heart Disease

The risk of coronary heart disease in patients with cholesterol levels of ____________ is 3 to 4 times greater than that in patients with levels less than _________

Incidence of CAD is lower in?

A

The risk of coronary heart disease in patients with cholesterol levels of 5.2 mmol/L is three to four times greater than that in patients with levels less than 4 mmol/L.

blood cholesterol level increases, incidence of death and disability related to CAD also increases

incidence of CAD is lower in premenopausal women

The goal of treatment is primary prevention and secondary prevention

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11
Q

Dyslipidemias and Treatment Guidelines

A

Canadian Cardiovascular Society Guidelines for the Diagnosis and Treatment of Dyslipidemia for the Prevention of Cardiovascular Disease in the Adult

Framingham Risk Score

Heart Age Calculator

Medications to treat dyslipidemia

Drug choice based on the specific lipid profile of the patient (phenotyping)

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12
Q

Hyperlipidemias Treatment and Guidelines

A

All reasonable non-drug means of controlling blood cholesterol levels (e.g., diet, exercise)

Drug therapy based on the specific lipid profile of the patient (age, sex, menopausal status)

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13
Q

Antilipemics

4 established classes of drugs

A

Hydroxymethylglutaryl–coenzyme A (HMG–CoA) reductase inhibitors (statins)

Bile acid sequestrants

B vitamin niacin (vitamin B3, nicotinic acid)

Fibric acid derivatives (fibrates)

Cholesterol absorption inhibitor (Ezetrol®)

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14
Q

Antilipemics:
Statins

Indications

A

First-line therapy for hypercholesterolemia (elevated LDL-C)

Treatment of type IIa and IIb dyslipedemia which reduces LDL-C levels

Reduces plasma concentrations of LDL cholesterol by 30 to 40%

Decrease in plasma triglycerides by 10 to 30%

Increase in HDL cholesterol by 2 to 15% > reduces cardiac risk

Dose dependent

takes 6-8 weeks to work

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15
Q

Antilipemics: HMG-CoA Reductase Inhibitors (Statins)

FACT

2 medications

A

Most potent LDL reducers

atorvastatin (Lipitor®)- effective at lowering triglycerides than other statins

rosuvastatin calcium (Crestor®)- more potent on a per mg basis. Used to replace atorvastatin due to AE of it. Has fewer AEs, and improved lipid profile

Other:
pravastatin sodium- administered in its active form
simvastatin (Zocor®)- prodrug
fluvastatin sodium (Lescol®)
lovastatin- prodrug

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16
Q

HMG-CoA Reductase Inhibitors: (Also known as Atorvastatin/ statins)

Mechanism of Action

A

Lower blood cholesterol levels by decrease rate of cholesterol production

(to produce cholesterol, the liver needs HMG-CoA reductase. The statins inhibits this enzyme, which decreases cholesterol production)

When less cholesterol is produced, the liver increases the number LDL receptors to recycle LDL from circulation
—-Needed for synthesis of steroids, bile, cell membranes

inhibit HMG-CoA reductase

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17
Q

HMG-CoA Reductase Inhibitors:

Adverse Effects

A

Mild, transient gastrointestinal disturbances

Rash

Headache

Elevation in liver enzymes

Myopathy (muscle pain), possibly leading to rhabdomyolysis, a serious condition

memory loss, confusion, forgetfulness, increased risk for hyperglycemia and Type 2 diabetes

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18
Q

Statins: Do not use for patients with?

A

Do not use for patients with elevated liver enzymes or liver disease

contra- allergy and pregnancy, high alcohol intake

previous myopathy/ rhabdomyolysis

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19
Q

Rhabdomyolysis

How to reverse it?

Instruct patients to report?

RF

A

Breakdown of muscle protein, accompanied by myoglobinuria (urinary elimination of muscle protein- myoglobin). This may strain the kidney and result in acute kidney injury.

Early detection- usually reversible with discontinuation of the statin drug

Instruct patients to immediately report any signs of toxicity, including muscle soreness or changes in urine colour (tea-coloured).

RF of myopathy- age older than 65, Asian descent hypothyroidism, immunosuppressant….

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20
Q

Myoglobinuria

Define

Can lead to?

A

urinary elimination of the muscle protein myoglobin

Can lead to acute kidney injury and even death

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21
Q

HMG-CoA Reductase Inhibitors:

Interactions

A

Oral anticoagulants

Drugs metabolized by CYP3A4

[erythromycin
azole antifungals
quinidine sulphate
verapamil hydrochloride
diltiazem hydrochloride
Human immunodeficiency virus (HIV) and hepatitis C protease inhibitors
amiodarone hydrochloride
Grapefruit juice
cyclosporine
clarithromycin
amlodipine]

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22
Q

atorvastatin calcium (Lipitor®) and rosuvastatin (Crestor®)

Mechanism of action

Dosing?

FACT

A

Lowers total and LDL-C 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

Two of the most commonly used drugs in this class of cholesterol-lowering drugs

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23
Q

rosuvastatin

A

Lowers total and LDL-C cholesterol levels as well as triglyceride levels. Can modestly raise HDL levels.

Use of 40 mg is contraindicated in the Asian population or in pts with myopathy/ rhabdomyolysis

24
Q

Bile Acid Sequestrants

1 medication

A

cholestyramine resin (Olestyr®)

Other:
colestipol hydrochloride
colesevelam
Also called bile acid–binding resins and ion-exchange resins

25
Q

Bile Acid Sequestrants: (bile acid-binding resins/ ion-exchange resins)

Mechanism of Action?

Bile acids are necessary for?

The more the bile acids are excreted, the more the liver converts?

Commonly used as?

A

Bind bile and prevent the resorption of bile acids from small intestine (bile acids are necessary for the absorption of cholesterol from the SI and are synthesized from cholesterol in the liver; the natural way the liver excretes cholesterol from the body). The more bile acids are excreted in the feces, the more the liver converts cholesterol to bile acids. This reduces the level of cholesterol in the liver and the circulation. LDL is released to compensate and it bind to receptors and is taken up by the liver- reducing circulating LDL in the blood

Lower cholesterol, (esp. LDL-C) by increasing the destruction of LDL

Bile acids are necessary for absorption of cholesterol.

The more the bile acids are excreted, the more the liver converts cholesterol to bile acids, reducing cholesterol in liver and circulation

Commonly used as an adjunct to statin therapy

26
Q

Bile Acid Sequestrants: Indications

A

Type II hyperlipoproteinemia

Relief of pruritus associated with partial biliary obstruction (cholestyramine)

May be used along with statins

27
Q

Bile Acid Sequestrants: Adverse Effects

A

Constipation

Heartburn, nausea, belching, bloating

—These adverse effects tend to disappear over time.
—-Increasing dietary fibre intake or taking a fibre 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

28
Q

Bile Acid Sequestrants: Considerations

A

Overdose can cause obstruction because the bile acid sequestrants are not absorbed.

Treatment of overdose includes restoring gut motility.

Take other drugs at least 1 hr before or 4-6 hrs after bile sequestrants

29
Q

Bile Acid Sequestrants: Drug interactions

A

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).

30
Q

Bile Acid Sequestrants: cholestyramine resin (Olestyr®)

Contraindications?

A

Contraindications: known hypersensitivity, phenylketonuria or complete biliary obstruction

Pregnancy and lactation considerations

Treatment of loose bowel movements

Caution when administering dry powder

interfere with the distribution of fat soluble vitamins

used for constipating effect, given for loose BMs

31
Q

Niacin (Niaspan®, nicotinic acid)

Type of vitamin?

A

Vitamin B3

32
Q

Niacin (Niaspan®, nicotinic acid)

Mechanism of action

Benefits?

Often given as?

A

Lipid-lowering properties require much higher doses than when used as a vitamin.

Effective, inexpensive, often used in combination with other lipid-lowering drugs

Often given as adjunct to statins

33
Q

Niacin: Mechanism of Action

A

inhibit lipolysis in adipose tissue

decrease esterification of triglycerides in the liver

increase the activity of lipoprotein lipase

Reduces the metabolism or catabolism of cholesterol and triglycerides

Resultant effect: decreased triglyceride levels, decreased LDL and increased HDL levels

May also stimulate fibrinolytic system to break down fibrin clots

34
Q

Niacin: Indications

A

Effective in lowering triglyceride, total serum cholesterol, apolipoprotein B and

LDL cholesterol levels
Increases HDL levels
Therapeutic effects noticed after 1-4 days of therapy

Maximum effects in 3-5 weeks of continuous therapy

35
Q

Niacin Contraindications

A

Contraindicated in peptic ulcer disease, hypertension, active hemorrhagic process

liver disease, allergy

36
Q

Niacin:

Adverse Effects

Contraindication

A

Flushing (caused by histamine release)

Pruritus

Gastrointestinal distress

start on low dosage, take with meals

small dose of aspirin (NSAID) may be taken 30 minutes before nicotinic acid to minimize cutaneous flushing

contra- statins- increase risk for myopathy, allergy, peptic ulcer, liver disease, hemorrhage, hypotension, lactating women, gout

37
Q

Fibric Acid Derivatives

Also known as?

1 medication

A

Also known as fibrates

gemfibrozil- decreases synthesis of Apo-B and lowers the VLDL level, increase HDL level, lower plasma triglyceride levels

Other:
bezafibrate
fenofibrate

38
Q

Fibric Acid Derivatives: Mechanism of Action

A

Activates lipoprotein lipase, which breaks down cholesterol

Suppress the release of free fatty acid from adipose tissue

Inhibit the synthesis of triglycerides in the liver

Increase the secretion of cholesterol in bile

can induce changes in blood coagulation; decrease in platelet adhesion

(can increase plasma fibrinolysis the process that causes fibrin (clots) to be broken down

decrease triglyceride levels and increase HDL levels; treats dyslipidemia

39
Q

Fibric Acid Derivatives: Indications

A

Treatment of types III, IV, and V hyperlipidemias

The fibric acid derivatives bezafibrate, gemfibrozil, and fenofibrate decrease the triglyceride level and increase the HDL cholesterol level by as much as 25%.

40
Q

Fibric Acid Derivatives: Contraindications

A

Known drug allergy

Severe liver or kidney disease

Cirrhosis

Gallbladder disease

use birth control- childbearing year and d/c in pregnant women

41
Q

Fibric Acid Derivatives: Adverse Effects

A

Abdominal discomfort, diarrhea, nausea

Blurred vision, headache

Increased risk of gallstones

Prolonged prothrombin time

Increased enzyme levels perhaps shown by liver studies

42
Q

Fibric Acid Derivatives: Interactions

A

Gemfibrozil enhances the action of oral anticoagulants (warfarin)

All are given with a statin, which increases risk of myositis, myalgia, and rhabdomyolysis.

43
Q

Fibric Acid Derivatives: Laboratory test reactions:

A

Decreased hemoglobin level, hematocrit value, and white blood cell count

Increased aspartate aminotransferase, activated clotting time, lactate dehydrogenase level, and bilirubin level

44
Q

Cholesterol Absorption Inhibitor

1 medication

A

ezetimibe (Ezetrol)

45
Q

Cholesterol Absorption Inhibitor

ezetimibe (Ezetrol)

Mechanism of action

A

Selectively inhibits absorption of cholesterol and related sterols from the small intestine

Results in reduced total cholesterol, LDL cholesterol, apolipoprotein B, and triglyceride levels

Also increases HDL cholesterol levels

Often combined with a statin drug

Can be used as monotherapy

Levels are increased by fibric acid derivatives- concurrent use is not recommended

contra- allergy, active liver disease

46
Q

Herbal Product: Garlic

Indications?

Adverse effects?

Interactions?

May enhance?

A

Used as an antispasmodic, antiseptic, antibacterial, antiviral, antihypertensive, antiplatelet, and lipid reducer
Adverse effects: dermatitis, vomiting, diarrhea, anorexia, flatulence, antiplatelet activity
Possible interactions with warfarin, diazepam, and protease inhibitors
May enhance bleeding when taken with nonsteroidal anti-inflammatory drugs (NSAIDs)

47
Q

Herbal Product: Flax

Types used?

Indication?

Adverse effect?

Interactions?

A

Both the seed and oil of the plant are used.

Uses: atherosclerosis, hypercholesterolemia, hypertriglyceridemia, gastrointestinal distress, menopausal symptoms, bladder inflammation, others

May cause diarrhea and allergic reactions
Possible interactions: antihyperglycemic drugs, anticoagulant drugs

48
Q

Herbal Product: Omega-3Fatty Acids

Type?

Indication?

Adverse effects?

Interactions?

Contraindicated?

A

Fish oil products

Used to reduce cholesterol

May cause rash, belching, allergic reactions

Potential interactions with anticoagulant drugs

Contraindicated in pregnancy

49
Q

Nursing Implications

A

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.

Obtain results of baseline liver function studies.

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.

Provide teaching regarding the use of NSAIDs and aspirin.

Inform patients that these medications may take several weeks to show effectiveness.

Instruct patients to report persistent gastrointestinal 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

50
Q

Antilipemic drugs contraindications?

Patients on long-term therapy may need supplemental?

How to take powder forms?

Other medications should be taken_____ before or 4___ to ___ hours after meals to avoid interference with ______.

To minimize adverse effects of ____, start on a low initial dose and gradually increase it, and have the patient take the medication with meals.

Small doses of ___ or ____ may be taken 30 minutes before ____ to minimize cutaneous flushing.

A

Contraindications include biliary obstruction, liver dysfunction, and active liver dysfunction

Patients on long-term therapy may need supplemental fat-soluble vitamins (A, D, E, K).

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 a low initial dose and gradually increase it, and have the patient take the medication with meals.

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

51
Q

cholesterol

chylomicrons

HMG-CoA

Lipoprotein

triglycerides

A

a fat-soluble steroid alcohol, widely distributed in the body (bile, blood, brain tissue, liver, kidneys, adrenal gland, myelin sheath)

carry fat to tissues, primarily in the liver

cholesterol-lowering drugs, act by inhibiting the rate-limiting step in cholesterol synthesis (statins)

conjugated protein synthesized in the liver that contains varying amounts of triglycerides, cholesterol, and other lipids

consist of fatty acids and a type of alcohol known as glycerol

52
Q

Lipid abnormalities (lipids and lipoprotein forms…)

foam cells

what causes atherosclerosis

Where does lipid metabolism occur?

A

atherosclerotic plaque which leads to CAD

lesion of atherosclerosis

repeated; injury to artery wall such as smoking, elevated BP, diabetes, elevated cholesterol. Ongoing inflammatory response has a central role in the formation of plaque referred to as atherogenesis.

Liver

53
Q

Risk factors for CAD

A

males 40 years or older

females 50 years or older or postmenopausal

family history, premature CAD

cigarette smoking

BP 140/90

low HDL

diabetes

54
Q

To know

A

Cholestyramine- test for PKU; pts with PKU cannot process amino acid phenylalanine (a protein component). High levels result in behavioural, cognitive, and learning dysfunction (child). for adults to monitor PKU monthly (dissolve it for 1 minute). Give 1 hour before or 4-6 hrs after other meds. Take with meals

statins- not for pts with liver disease, who drink alcohol because of potential liver dysfunction- assess liver tests. Take with 120-180 mL of water or with meals. Monitor liver and kidney function every 3-6 months.

nicotinic- contra in active bleeding. flushing of face may occur, take the drug with meals. Monitor liver, kidney , and PThrombin. Take with meals.

antilipemic- may require supplementation of vitamins, GI problems, and liver dysfunction.

low fat, low cholesterol diet (diet rich in raw veggies, fruit, and bran) Incase fluids.

55
Q

Never take dry form of

A

powder/ granule , oral-based form of antilipemic- must be mixed with carbonated liquids

56
Q

Lipids and lipoprotein

A

participate in the formation of A plaque which leads to CAD

when plaque forms in the BVs that supply the heart with oxygen and nutrients, the lumen will decrease and 02 and nutrients supplied will also be reduced

57
Q

How to lessen AE of nitric acid

Monitor this when giving nitric acid

Report muscle pain when taking

contraindication of antilipemics

what drug puts a pt at a higher risk for developing rhabdomyolysis?

cholestyramine (Bile a cid sequestrant) nursing interventions?

lab tests for statins

A

administer a small dose of aspirin or an NSAID 30 minutes before niacin dose

cutaneous flushing

statins

liver cirrhosis

fibric acid derivatives

take with meals, take fibre supplements, increase fluids, not take with other drugs

total cholesterol, triglycerides, liver function tests, HDL &LDL levels

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