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Pharmacology: Exam 3 > Lecture 4: Antihyperlipidemics > Flashcards

Lecture 4: Antihyperlipidemics Flashcards

1
Q

What does the drug classes of Antihyperlipidemics treat?

A

Dyslipidemia or Increases HCl

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2
Q

Which drug(s) are HMG-CoA reductase inhibitors (5)?

Drug class

All end in -statin

A
  • Atorvastatin
  • Rosuvastatin
  • Simvastatin
  • Pravastatin
  • Lovastatin
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3
Q

Which drug(s) are Lipolysis inhibitors?

Drug class

A
  • Niacin
  • Nicotinic acid
  • Vitamin B3
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4
Q

Which drug(s) are Fibrates?

Drug class

A
  • Gemfibrozil
  • Fenofibrate
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5
Q

Which drug(s) are Bile acid sequestrants?

Drug class

A
  • Cholestyramine
  • Colestipol
  • Colesevelam
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6
Q

Which drug(s) are Cholesterol absorption inhibitors?

Drug class

A

Ezetimibe

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7
Q

Which drug(s) are Triglyceride transfer protein inhibitor?

Drug class

A

Lomitapide

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8
Q

Which drug(s) are PCSK9 inhibitor?

Drug class

A

Evolocumab (monoclonal antibody)

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9
Q

Which drug(s) are Fish oils?

A

Omega-3-acid ethyl esters

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10
Q

Which drug(s) are ATP Citrate Lyase Inhibitor?

Drug class

A

Bempedoic acid

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11
Q

Which drug(s) are siRNA?

Drug class

A

Inclisiran

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12
Q

What accounts for 50% of all deaths in the USA?

A

Coronary heart disease (CHD)

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13
Q

What does CHD correlate with regarding cholesterol?

HIGH yield

A
  • ↑ LDL (bad chol) and TAG
  • ↓HDL (good chol)

  • LDL&HDL=carriers of cholesterol (chol)
  • TAG=triacylgcerol
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14
Q

What are other risk factors of CHD?

A
  • Smoking
  • Hypertension
  • Obesity
  • Diabetes mellitus (DM)
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15
Q

What causes high cholesterol?

A
  • ↓ excercise
  • ↑ saturated fatty acids
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16
Q

What is Hyperlipidemia?

HIGH yield

A

Genetic defect in lipoprotein metabolism

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17
Q

What is the treatment plan for hyperlipidmias and the proposed outcome?

A
  • Lifestyle changes + drugs (↓ coronary plagues)
  • ↓mortality of CHD≈35%
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18
Q

True or False? Antihyperlipidemics are taken chronically

A

TRUE
(do Not cure, just manage and alleviate)

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19
Q

List the lipoprotein in order of clinical importance (according to atherogenicity)

A

LDL>VLDL>chylomicrons>HDL

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20
Q

What is the amount of LDL present that is associated with CHD?

A

100 (↑LDL)

High LDL and low HDL are both risk factors for CHD

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21
Q

What is the amount of HDL needed to decrease heart disease risk?

A

40 (↑HDL)

Note: If HDL gets too low can cause CHD

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22
Q

What is the primary goal of anthyperlipidemic therapy?

A

the lower LDL levels

More aggresive therapy for pts with ↑ risk of heart disease

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23
Q

What are the components of the Total Cholesterol (Below 200) in a healthy individual?

A

HDL (>40) + LDL (<100) + VLDL

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24
Q

What is the intitial treatment guidline for a patient w/ high cholesterol?

2018-19 ACC/AHA Guidelines on the Management of Blood Cholestrol

A

Healthy lifestyle (e.g. diet, exercise, emphasized over the entire course of life)

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25
Q

What is the treatment guildline for a patient w/ Clinical Atherosclerosis Cardio Disease (ASCVD)?

2018-19 ACC/AHA Guidelines on the Management of Blood Cholestrol

A
  • ↓ LDL by ≥ 50% w/ high-intesity statin (Atrovastatin/Rosuvastatin)
  • Add nonstatain when LDL ≥ 70 mg/dL (Ezetimibe/Cholestyramin)
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26
Q

What is the treatment guidelines for a Pt w/ Severe hypercholesterolemia (LDL≥190 mg/dL) ?

2018-19 ACC/AHA Guidelines on the Management of Blood Cholestrol

A
  • High intensity statin at highest tolerated dose (Atrovastatin/Rousvastatin)
  • Add a nonstatin, If LDL ≥ 100 mg/dL in high-risk Pt
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27
Q

What is treatment guideline for a Pt w/ DM + LDL>70 mg/dL), 40-50 y/o?

DM-Diabetes mellitus

2018-19 ACC/AHA Guidelines on the Management of Blood Cholestrol

A
  • Moderate-intensity statin
  • Considered to ↓ LDL by ≥ 50% in Pt at high risk
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28
Q

What is the treatment guildline for a Pt w/ 10 year ASCVD risk≥7.5%, 40-75 y/o?

2018-19 ACC/AHA Guidelines on the Management of Blood Cholestrol

A
  • Consider moderate-intensity statin
  • Discussion of risk enhacing factors and coronary artery Ca
  • Can ↓LDL by ≥ 30% to 50% if 10 year risk ≥20%
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29
Q

Which statins are High-Intensity (daily dose ↓ LDL by ≥ 50%)?

HIGH yield

A
  • Atorvastatin: 40-80 mg
  • Rosuvastatin: 20 mg
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30
Q

Which statins are Moderate-intensity (daily dose ↓ LDL by 30-50%)?

A
  • Atrovastin: 10 mg
  • Rousuvastatin: 10 mg
  • Simvastatin: 20-40 mg
  • Pravastatin: 40 mg
  • Lovastatin: 40 mg
  • Fluvastatin: 40 mg (BID)
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31
Q

Which statins are Low-intensity (daily dose ↓ LCL by < 30%)?

HIGH yield

A
  • Pravastatin: 10-20 mg
  • Lovastatin: 20 mg
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32
Q

Explain the mechanism of action of Statins

ALL of the statins do this

A
  • Analogs of HMG (3-OH-3-CH3-glutaryl), a cholesterol precursor
  • Inhibit HMG CoA reductase, rate-limiting step in cholesterol synthesis
  • Inhibit de nevo cholesterol synthesis→deplete intracellular supply of cholesterol
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33
Q

Rank the statin order potency of LDL lowering power

A

Pitavastatin, Rosuvastatin, Atorvastatin > Simvastatin, Pravastatin > Lovastatin, Fluvastatin

34
Q

Explain the mechanism of statins step by step

Review Slide 13

A
  1. Statins inhibit HMG-CoA reductase, leading to a decreased concentration of cholesterol within the cell
  2. Low intracellular cholesterol stimulates the synthesis of LDL receptors
  3. Increased number of LDL receptors on the cell promotes the uptake of LDL from the blood
  4. Low intracellular cholesterol decreases the secretion of VLDL
35
Q

Explain the mechanism of action for Atrovastatin

A
  • Depletion of intracellular cholesterol→ ↑ LDL receptors →bind & internalize circulating LDL
  • ↓ LDL (24-50%) by decreasing synthesis & increasing catabolism
  • ↑ HDL (6-12%)
  • ↑ TAG (10-29%)
36
Q

What are the therapeutic uses of Atrovastain?

A
  • Treatment of hyperlipidemia
  • Substantial ↓ coronary events & death from CHD
  • Plaque stabilization
  • Improve coronary endothelial function
  • ↓ Clot formation, anti-inflammatory effect
37
Q

List specific conditions that Atrovastain therapy is benefical

A
  • CHD w/ or w/out hyperlipidema
  • Males with hyperlipidema w/ out CHD
  • Male and female with average cholesterol w/ out CHD
38
Q

What disease is Atrovastatin treatment NOT effective and why?

A

Homozygous familial hypercholesterolemia d/t lack of functional LDL receptors

39
Q

List the different side effects that can be caused by Atorvastatin

HIGH yield

A
  • Constipation (10%)
  • Muscle aches (1%)
  • Hepatotoxicity (0.001%)
  • Myositis or Rhabdomyolysis (<0.1%)
  • DM (0.2% risk/yr)
  • Confusion/Memory impairment
  • Contraindicated in pregnancy
40
Q

What drugs do you NOT take w/ Atrovastatin and why?

HIGH yield

A
  • Gemfibrozil and Niacin
  • Overlapping side effects can lead to liver and kidney failure
41
Q

List other drug interactions w/ Atrovastin

A
  • Cylosporine
  • Itraconazole
  • Erythromycin
42
Q

A 43-year-old obese man with type 2 diabetes mellitus is prescribed atorvastatin for the treatment of hyperlipidemia. Which of the following is the mechanism of action of atorvastatin?
A. Triacylglycerol secretion inhibitor
B. HMG-CoA reductase inhibitor
C. Cholesterol absorption inhibitor
D. Cholesterol secretion inhibitor

A

B. HMG-CoA reductase inhibitor

43
Q

What type of drug is Niacin?

A

Lipolysis inhibitor

44
Q

Explain the mechanism of action of Niacin

A
  • Inhibits TAG lipolysis in adipose tissue
  • TAG is primary FA source
  • Liver utilizes FA for TAG synthesis
  • ↓ TAG synthesis → ↓VLDL →↓ LDL
  • ↑ HDL by↓ its catabolism
  • ↑ Tissue plasminogen activator, ↓ fibrinogen
  • Reverse some endothelial cell dyfxn, contributing to clots w/ hypercholesterolemia & atherosclerosis
45
Q

What are the therapeutic uses of Niacin?

A
  • Treatment of hyperlipidemia
  • ↓LDL (15-25%), ↑ HDL (25-35%) the most
46
Q

List the side effects that can be caused by Niacin

HIGH yield

A
  • Flushing ( ↓w/ ASA, IBU)
  • Pruritis
  • N/V
  • Hepatitis (Niaspan®)
  • Hyperuricemia (gout)
  • Hyperglycemia (DM)
47
Q

Explain the pharmacokinetics of Niacin

A

Converted into nicotinamide which has no activity

48
Q

Drug interactions

What drug should not be taken with Niacin and why?

HIGH yield

A

Statins: ↑ muscle & liver toxicity risk

49
Q

Explain the mechanism of action of Gemfibrozil

A
  • Peroxisome proliferator-activated receptor-α (PPAR-α) agonists
  • PPAR-α –Transcription factor that regulates lipid metabolism
  • ↓ TAG (40%) → lipoprotein lipase (TAG→FA)
  • ↑HDL (15-20%) → ↑apo A-I/II
  • ↓ LDL (10-15%)
50
Q

What are the therapeutic use(s) of Gemfibrozil?

A

Treatment of hyperlipidemia

51
Q

List the side effects that can be caused by Gemfibrozil

A
  • Hepatitis
  • Myositis (weakness, stiffness)
  • Gallstones (↑ bilary cholesterol excretion)
52
Q

What drug should not be taken with Gemfibrozil and why?

A
  • ↑Warfarin INR
  • Statins: ↑ muscle & liver toxicity risk
53
Q

What is the mechanism of action of Cholestyramine?

Bile acid sequestrants

A
  • Anion exchange resins which bind (-) charged bile acids & salts in small intestines
  • Resin/bile acid complex excreted in feces
  • Inhibiting entereohepatic recycling (gets rid of bile acid)
  • ↓ bile acids→liver →cholesterol→bile acids
  • ↓ Intracellular cholesterol→liver→ ↑LDL uptake via cell surface receptors
  • ↓plasma LDL (10-25%) & ↑ HDL (5-10%)
54
Q

List the therapeutic uses and side effects of Cholestyramine

A
  • Therapeutic use
    1. Treatment of hyperlipidemia
    2. Little effect in patients lacking functional LDL receptors
  • Side effects:
    1. Constipation
    2. N/V
    3. Flatulence

N/V=Nausea/Vomiting

55
Q

What are the drug interactions of Cholestyramine?

A

Acidic drugs, e.g., Warfarin, Niacin, Digoxin & Vitamins A, D, E, K

Interferes w/ absorption

56
Q

What is considered the safest class of lipid-modifying drugs during pregnancy?

HIGH yield

A

Cholestyramine

57
Q

What is the mechanism of action of Ezetimibe?

Cholesterol absorption inhibitors

A
  • Inhibits cholesterol absorption at the brush border of the intestines & liver, ↑ LDL-R expression
  • ↓ in cholesterol stores→ ↓ plasma cholesterol
  • ↓ LDL (15-20%), ↓ TAG (6%), ↑ HDL (5%)
58
Q

List the therapeutic uses and side effects of Ezetimibe

A
  • Therapeutic use
    1. Treatment of Hyperlipidemia
  • Side effects:
    1. GI upset

Pharmacokinetics: UGT

59
Q

What drug class has the greatest effects on decreasing LDL?

A

Statins

60
Q

What drug class has the greatest effects on decreasing TAG?

A

Fibrates (Gemfibrozil)

61
Q

What drugs class has the greatest effect on increasing HDL?

A

Niacin

62
Q

What is the mechanism of action of Lomitapide?

Microsomal triglyceride transfer protein inhibitoes

A
  • Microsomal triglyceride transfer protein inhibitor
  • Prevents assembly of apo-B containing lipoproteins (chylomicrons & VLDL in liver & GIT)
  • ↓ plasma LDL concentrations
63
Q

List the therapeutic use and side effects of Lomitapide

A
  • Therapeutic use
    1. !!Treatment of homozygous familial hypercholesterolemia!!
    2. As an adjunct to lipid-lowering medications & diet
  • Side effects:
    1. LFT
    2. FDA Pregnancy Category X

Pharmacokinetics: CYP3A4 substrate: DI, Hepatic dysfunction

64
Q

What is the mechanism of action of Evolocumab?

PCSK9 inhibitor

A
  • Selectively binds to PCSK9 & prevents PCSK9 from degrading LDL receptors in hepatocyte lysosomes which ↑ # of recycled LDL receptors
  • ↑ # of LDL receptors → ↓ LDL plasma concentrations
65
Q

List the therapeutic uses and side effects of Evolocumab

A
  • Therapeutic use:
    1. heterozygous or homozygous familial hypercholesterolemia
    2. Atherosclerotic cardiovascular disease
    3. Adjunct to Diet + Statin therapy
  • Side effects:
    1. Nasopharyngitis
    2. Upper respiratory tract infection
    3. Flu
    4. Back pain
    5. Allergic reactions
    6. Injection site rxns (redness, pain, or brushing)
66
Q

List examples of Omega-3-acid ethyl esters

A
  • EicosaPentAenoic (20:5)-EPA
  • DocosaHexAenoic acids (22:6)-DHA
67
Q

What is the mechanism of action of Omega-3-acid ethyl esters?

Fish oils

A
  • Activation of nuclear transcription factors (e.g., peroxisome proliferator-activated receptor-α (PPAR-α))
  • ↑ liver fatty acid oxidation → ↓ TAG synthesis
68
Q

List the therapeutic use(s) of omega-3-acid ethyl esters

A
  • Treatment of hyperlipidemia
  • ↓ TAG (14-30%), ↑ HDL (10%)
  • ↑ LDL (Icosapent [Pure prescription strength] the least)
69
Q

What are the side effects caused by omega-3-acid ethyl esters?

A
  • Thrombocytopenia
  • Halitosis
  • Dysgeusia
  • Dyspepsia
  • Infection
  • Back pain
  • Flu-like syndrome
70
Q

What is the mechanism of action for Bempedoic acid?

A
  • Inhibitor of ATP citrate lyase (Enzyme in de novo cholesterol synthesis)
  • ↑ LDL-R by ↓ cholesterol synthesis
  • Prodrug
  • Active metabolite produced in liver not muscle, Less muscle toxicity?
71
Q

What are the therapeutic use(s) of Bempedoic acid?

A

Adjunct to diet & max tolerated statin for heterozygous familial hypercholesterolemia or atherosclerotic cardiovascular

72
Q

List the side effects caused by Bempedoic acid?

A
  • Gout
  • Tendon rupture
  • Anemia
  • ↑ Liver enz
  • Muscle spasms
73
Q

Review Slide 40

A

Review Slide 40

74
Q

What is the mechanism of action Inclisiran?

siRNA

A
  • Small interfering RNA (siRNA) for PCSK9 mRNA
  • Inhibits PCSK9 synthesis
75
Q

What are the therapeutic use(s) and side effects of Inclisiran?

A
  • Therapeutic use
    1. Diet, Max Statin
    2. Heterozygous familial hypercholesterolemia
    3. Secondary prevention of cardiovascular events
  • Side effects:
    1. Antibodies
    2. Arthralgia (Joint pain)
    3. Bronchitis
76
Q

Which of the following is the most clinically important side effect of the Niacin sustained release dosage form (Niaspan®)?
A. Dermatitis
B. Meningitis
C. Nephritis
D. Hepatitis

A

D. Hepatitis

77
Q

Which of the following antihyperlipidemics effect TAG the greatest?
a. Gemfibrozil
b. Ezetimibe
c. Cholestyramine
d. Atorvastatin

A

a. Gemfibrozil

78
Q

Which of the following inhibits PCSK9 synthesis via siRNA
a. Inclisiran
b. Bempedoic Acid
c. Cholestyramine
d. Gemfibrozil

A

a. Inclisiran

79
Q

Which of the following is safest for pregnancy?
a. Atorvastatin
b. Niacin
c. Cholestyramine
d. Lomitapide

A

c. Cholestyramine

80
Q

Which of the following can treat homozygous hypercholesterolemia?
a. Lomitapide
b. Atorvastatin
c. Niacin
d. All of the above

A

a. Lomitapide

Pharmacology: Exam 3 (8 decks)

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