Updated: 8/6/2020

Asthma Drugs

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Overview
  • Therapeutic strategies for treating asthma include:
    • decreasing inflammation
    • increasing sympathetic tone
  • There are 7 families of drugs that are commonly used:
    1. corticosteroids
    2. β-agonists
    3. muscarinic antagonists
    4. methylxanthines
    5. cromolyn
    6. antileukotrienes
    7. omalizumab
Corticosteroids
  • Inhaled corticosteroids are first line therapy for chronic asthma 
  • Examples
    • mometasone
    • fluticasone 
    • budesonide
    • beclomethasone
    • triamcinolone
    • flunisolide
  • Mechanism
    • inhibiting the synthesis of virtually all cytokines
    • upregulating expression of beta-adrenergic receptors 
    • inactivating NF-κB
      • NF-κB is the transcription factor that induces the production of TNF-α and other inflammatory agents
  • Toxicity
    • oral candidiasis
      • use spacers or post-inhalation mouth rinse to prevent 
β2-agonists
  • Drugs
    • short acting -- used for breakthrough symptoms and during acute exacerbation
      • albuterol 
        • known internationally as salbutamol
      • levalbuterol 
      • Others used much less commonly
        • terbutaline
        • metaproterenol (β2, minor β1)
        • isoproterenol (nonselective)
          • tachycardia
          • may lead to cardiac death
    • long acting -- used for maintenance in combination with inhaled corticosteroid (never without)
      • salmeterol 
        • tremors, arrhythmia
      • formoterol 
  • Mechanism
    • β2 receptors are activated on bronchial smooth muscle to achieve bronchodilation
    • stimulation of adenylate cyclase leading to closing of calcium channels and ultimately the relaxation of smooth muscles
Methylxanthines
  • Drugs
    • theophylline (rarely used)
  • Mechanism
    • inhibition of phosphodiesterase leading to decreased cAMP hydrolysis
      • causes bronchodilation
    • metabolized by P-450
    • blocks actions of adenosine
  • Toxicity
    • seizures 
    • narrow therapeutic index
    • nausea/vomiting
    • arrhythmia
Muscarinic antagonists
  • Drugs
    • ipratropium 
    • tiotropium
  • Mechanism
    • competitive inhibition of muscarinic receptors 
      • prevents bronchoconstriction
  • Also used for COPD
Cromolyn
  • Prophylaxis only!
    • ineffective during an acute asthma attack
  • Mechanism
    • prevents release of mediators from mast cells
  • Toxicity
    • rare
Antileukotrienes
  • Drugs
    • zileuton
      • 5-lipoxygenase pathway inhibitor
        • blocks conversion of arachidonic acid to leukotrienes 
    • zafirlukast, montelukast
      • blocks leukotriene receptors
      • particularly effective in aspirin-induced asthma
Omalizumab
  • Clinical use
    • severe uncontrolled asthma with elevated IgE
      • symptoms and activity refractory to standard therapies and oral glucocorticoids
  • Mechanism
    • anti-IgE antibody  
      • inhibits action of IgE with inflammatory cells 
    • asthma can be caused by uncontrollably high IgE response
 

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Questions (12)
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(M1.PL.15.106) An 8-year-old female is given omalizumab for the treatment of bronchial asthma. Omalizumab treats asthma through which mechanism? Tested Concept

QID: 100909
1

Inhibition of IgE binding to mast cells

84%

(57/68)

2

Binding to nuclear receptors

4%

(3/68)

3

Inhibition of leukotriene binding to receptor

7%

(5/68)

4

Inhibition of phosphodiesterase breakdown of cAMP

3%

(2/68)

5

Mediating type IV hypersensitivity reaction

1%

(1/68)

M 1 D

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(M1.PL.14.33) In patients with chronic obstructive pulmonary disease, stimulation of muscarinic acetylcholine receptors results in an increase in mucus secretion, smooth muscle contraction and bronchoconstriction. The end result is an increase in airway resistance. Which of the following pharmacologic agents interferes directly with this pathway? Tested Concept

QID: 100836
1

Epinephrine

2%

(1/58)

2

Theophylline

2%

(1/58)

3

Ipratropium

88%

(51/58)

4

Albuterol

9%

(5/58)

5

Metoprolol

0%

(0/58)

M 1 E

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(M1.PL.14.41) A 7-year-old boy is brought to your office with complaints of wheezing and dyspnea. Laboratory work reveals eosinophilia and positive skin tests for allergens. Which of the following types of drugs would be an effective treatment in this patient? Tested Concept

QID: 100844
1

Beta-2 antagonist

16%

(27/167)

2

Histone deacetylase inhibitor

7%

(12/167)

3

VEGF inhibitor

5%

(8/167)

4

Muscarinic antagonist

71%

(119/167)

5

Anticoagulant

0%

(0/167)

M 3 E

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(M1.PL.13.126) A new drug is designed to treat asthma by inhibiting bronchoconstriction. Experimental assays show that treated animals had markedly reduced acetylcholine binding to muscarinic receptors relative to untreated controls. The drug is most similar to which of the following: Tested Concept

QID: 100929
1

Theophylline

8%

(5/64)

2

Cromolyn

0%

(0/64)

3

Zafirlukast

5%

(3/64)

4

Prednisone

2%

(1/64)

5

Ipratropium

84%

(54/64)

M 3 E

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(M1.PL.13.91) A 12-year-old female presents to her pediatrician with an asthma exacerbation. Upon physical examination, the physician notes the finding shown in Figure A. This presentation is a common side effect of which of the following pharmacologic agents used in the treatment of asthma? Tested Concept

QID: 100894
FIGURES:
1

Salmeterol

3%

(2/73)

2

Albuterol

5%

(4/73)

3

Inhaled beclomethasone

84%

(61/73)

4

Ipratropium

3%

(2/73)

5

Theophylline

4%

(3/73)

M 3 E

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Evidence (14)
Topic COMMENTS (8)
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