CVPR Week 5: Drugs used in the treatment of Asthma and COPD Flashcards

1
Q

β2 adrenergic agonists to know

3 listed

A
  • Albuterol
  • Terbutaline
  • Salmeterol
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2
Q

Muscarinic antagonists to know

2 listed

A
  • Ipratropium
  • Tiotropium
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3
Q

Phosphodiesterase inhibitors to know

2 listed

A
  • Theophylline
  • Roflumilast
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4
Q

Antileukotrienes to know

3 listed

A
  • Ziluteon
  • Zarfirlukast
  • Motelukast
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5
Q

Corticosteroids to know

2 listed

A
  • Beclomethasone
  • Fluticasone
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6
Q

Anti-IgE Antibodies to know

A

Omalizumab

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7
Q

Mast cell degranulation inhibitors to know

A

Cromolyn sodium

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8
Q

Anti-IL5 receptor antibody to know

A

Benralizumab

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9
Q

Hallmarks of asthma

9 listed

A
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10
Q

Hallmarks of COPD

8 listed

A
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11
Q

Hyperreactivity and hypersensitivity

A

sensitive to less stimulus

vs

the amount of smooth muscle contraction in response

Both are in asthma to cause Hyperresponsiveness

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12
Q

Normal control of bronchial tone

A
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13
Q

Treatment of asthma for hyperresponsiveness of the trachea and bronchi to stimuli and smooth muscle contraction

5 listed

A
  • β2-agonists
  • PDEi - Theophylline
  • Roflumilast
  • Antimuscarinics
  • Leukotriene modifiers
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14
Q

Treatment of asthma: Mucosal thickening from edema and mucus plug and cellular infiltration

6 listed

A
  • Corticosteroids
  • Leukotriene modulators
  • Mast cell stabilizer
  • Anti-IgE
  • Anti-IL5R
  • PDEi
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15
Q

Treatment of asthma: Short-term relief

A

bronchodilating agents to increase airway caliber by relaxing smooth muscles

  • β-adrenoreceptor agonists
  • Theophylline
  • Antimuscarinics
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16
Q

Treatment of asthma: Long-term control

A

Antiinflammatory agents to reduce edema, mucus and infiltration

  • Inhaled corticosteroids
  • Antileukotrienes
  • mast cell stabilizer (Cromolyn sodium)
  • Anti-IgE
  • β2 agonists
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17
Q

Bronchial tone

A
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18
Q

β2 adrenergic agonists properties

A
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19
Q

Effects of albuterol

A
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20
Q

Short-acting β2 agonists

A
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21
Q

Long-acting β2 agonists

A
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22
Q

What is the key to triggering the inflammatory cascade seen in asthma?

A
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23
Q

Anti-IL5 drugs

A

Benralizumab (Reslizumab and Mepolizumab bind IL-5

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24
Q

IL-5

A

Anti-IL-5 alpha chain receptor mAB IL-5 is a key cytokine in eosinophil maturation, activation, survival and proliferation

25
Q

Benralizumab in severe asthma

A

In severe eosinophilic asthma, Benralizumab decreased eosinophils in the airways, sputum, bone marrow and peripheral blood

26
Q

Benralizumab adverse effects

A

allergic hypersensitivity reactions (including anaphylaxis)

27
Q

Benralizumab clinical use

A
  • Add-on maintenance therapy
  • approved in ages 12 and older
28
Q

Antimuscarinics MOA in Asthma

A
29
Q

Antimuscarinics MOA in Asthma

A
30
Q

Antimuscarinic agents

A

Ipratropium bromide (Atrovent, atropine derivative) inhalation treatment for COPD

Tiotropium (Spiriva) a longer-lasting agent

31
Q

Antimuscarinic clinical uses

A
  • Inhibits bronchoconstriction
  • Inhibits tracheobronchial secretions
  • A weak bronchodilator
  • Used in asthma patients intolerant to
32
Q

Leukotriene antagonists and synthesis inhibitors

A
  • CysLTX - a role in airway remodeling
  • LTD4 and LTE4 - bronchial smooth muscle constriction
  • LTD4 is 1000x more potent than histamine
  • Zafirlukast and Montelukast are competitive antagonists
  • Zileuton is an inhibitor of 5-Lipoxygenase
  • Controlling drugs
33
Q

Leukotriene antagonists MOA

A
34
Q

Leukotriene modifying agents

A
35
Q

Zafirlukast toxicities

A
36
Q

Ziluteon warnings/precautions

A
37
Q

Methylxanthines MOA

A
38
Q

Methylxanthines

2 listed

A
  • Theophylline
  • Roflumilast
39
Q

Methylxanthines clinical uses

A
40
Q

Roflumilast MOA

A
41
Q

Roflumilast specific MOA

A

PDE type 4 inhibitor

42
Q

Roflumilast clinical uses

A

long acting PDE4 inhibitor (not considered a bronchodilator)

For severe COPD - controller not a rescue drug

43
Q

Roflumilast Interactions

A

Avoid in combination with CYP3A4/5 inhibitors or inducers (carbamazapine, cimetidine, erythromycin, fluvomoxamine, ketoconazole, phenytoin, rifampicin and some oral contraceptives)

44
Q

Roflumilast adverse effects

A
  • Can cause tachycardia like other PDE inhibitors
  • Some indication of depression
  • can cause muscle spasm and uncontrollable shaking
45
Q

Bronchodilators MOA

A
46
Q

Therapeutic treatment for the inflammatory side of asthma

A
47
Q

Corticosteroids Hx of Tx asthma

A

Used to treat asthma since 1950

48
Q

Corticosteroids for asthma

4 listed

A
  • Methylprednisone
  • beclomethasone
  • Fluticasone
  • Mometasone
49
Q

Corticosteroids clinical uses for asthma

5 listed

A
  • reduces bronchial reactivity
  • increases airway caliber
  • Increases β2 receptors
  • Inhibit production of LTX, PGs and PAF
  • By repressing gene transcription - interferring with Nfkappa B transcriptional regulation of cytokine production, represses transcription of NOSi, COX-2, cytokine receptors
50
Q

Corticosteroids MOA

A
51
Q

Rate of death from Asthma to Corticosteroids used

A
52
Q

Cromolyn sodium clinical uses

A

only valuable prophylactically

Inhibit antigen (seasonal or situational) and exercise induced asthma

No effect on airway smooth muscle tone

Does not reverse bronchospasm

Should not be used during an acute asthmatic episode

53
Q

Cromolyn sodium MOA

A
  • Cromolyn sodium alters chloride channel function which inhibits Ca2+ influx thus inhibiting mast cell function and airway nerves
  • In the mast cell this prevents the release of histamine and LTX
  • May also inhibit the function of other inflammatory cells
54
Q

Omalizumab MOA

A
55
Q

Omalizumab clinical use

A
  • administered over 10 weeks for those with poorly controlled or severe asthma
  • Reduces magnitude of early and late bronchospasms responses
56
Q

Omalizumab adverse effects

A

Anaphylaxis

57
Q

Omalizumab malignancies

A

breast

non-melanoma skin

prostate

melanoma

parotid

58
Q

Omalizumab infections

A

geohelminthic infections (roundworm, hookworm, whipworm, threadworm)

59
Q

Cromolyn sodium, benralizumab, omalizumab MOA

A