CHAPTER 32
Bronchodilator Drugs
and the Treatment
of Asthma
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Common Diseases Affecting
the Respiratory Tract
• Chronic bronchitis – condition caused by
chronic respiratory irritation, inflammation, and
characterized by increased secretions and
infection (COPD) smoking
• Emphysema – disease characterized by
destruction of alveoli, labored respiratory gas
exchange, and shortness of breath (↓exhale)
• Asthma – inflammatory disease of the
respiratory passageways characterized by
bronchoconstriction and shortness of breath
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Emphysema
• Destruction of alveolar walls – dose
dependently related to smoking
• Limits exercise tolerance – requires
supplemental O2
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Asthma
• 5% of US population – 5000 deaths / y
• Bronchoconstriction – reversible smooth
muscle contraction – controlled by
– Contraction - parasympathetic – AC
– Dilation – sym – β2 adrenergic receptor
• Inflammation of bronchiolar mucosa
• Shortness of breath, cough, wheezing,
smothering feeling, mucous secretion
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COPD
• Affects 20% of Us pop.
• Secondary to smoking “mucous escalator”
• Combination of chronic bronchitis and
emphysema irreversible, progressive does
respond to treatment
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Inflammatory Mediators
of the Respiratory Tract
• Histamine
• Eosinophilic chemotactic factor of
anaphylaxis (ECF-A)
• Prostaglandins and leukotrienes
• Slow-reacting substance of anaphylaxis
(SRS-A)
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Autonomic Control
of the Respiratory Tract
• Bronchiolar smooth muscle is relaxed by
beta-2 adrenergic receptor stimulation
• Bronchiolar smooth muscle is contracted
by cholinergic receptor stimulation
• Respiratory secretions are increased by
cholinergic stimulation
• Drugs that increase intracellular levels of
cyclic AMP produce bronchodilation
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Bronchodilator Drugs
• Sympathomimetics – drugs that stimulate
beta-2 adrenergic receptors
• Xanthine derivatives – theophylline
• Parasympatholytics – drugs that block
cholinergic receptors (anticholinergic
drugs)
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Bronchodilators
• Short acting – “rescue inhalers” 4-6 hr
– Terbutaline (Brethine)
– Albuterol (Proventil)
• Long acting – 12 hr
– Salmeterol (Severent)
• Drugs of choice for mild asthma
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Beta Adrenergic Drugs
• Epinephrine and isoproterenol are nonselective
beta-1 and beta-2 agonists
• Albuterol, terbutaline, and salmeterol are
selective beta-2 agonists that do not cause
excessive cardiac stimulation
• Selective beta-2 drugs are preferred for the
control of asthma
• Epinephrine SC is the drug of choice to treat an
acute attack of asthma
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Theophylline
• Increases cyclic AMP levels to cause
bronchodilation and inhibition of chemical
mediator release from mast cells
• Theophylline is usually administered orally
• In COPD theophylline decreases
secretions and stimulates respiration
• Overdosage produces cardiac and CNS
stimulation, and may cause seizures
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Corticosteroids
• Drugs of choice for moderate – severe
asthma
• Anti-inflammatory – decrease airway
lymphocytes & eosinophills - no effect on
muscle spasm
– Mucosal edema
– Leukotriene secretion
– Mucous secretion
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Corticosteroids
• Given by aerosol BID-QID
• Must use a “spacer” – prevents thrush
• Beclomethasone (Vanceril)
• Budesonide (Pulmocourt)
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Corticosteroids
• Adrenal gland hormone derivatives used in
inflammatory and allergic conditions
• Administered orally or parenterally in acute
asthmatic and inflammatory diseases
• Administered by oral inhalation for the
chronic control of asthma and related
inflammatory conditions
• Inhalation limits systemic toxicity
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Anticholinergic Drugs
• Ipratropium bromide (Atrovent) is the only
drug currently available
• By blocking cholinergic receptors
ipratropium produces bronchodilation and
decreased respiratory secretions
• The drug is administered by oral inhalation
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Leukotrienes Inhibitors
• Anti-inflammatory drugs that interfere with
the inflammatory actions of the
leukotrienes
• Zafirlukast (Accolate) and montelukast
(Singulair) block leukotriene receptors
• Zileuton (Zyflo) blocks the enzyme
required for the formation of leukotrienes
• Drugs are indicated for the chronic
treatment and control of asthma
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Ant allergic Drugs
• Cromolyn and nedocromil (Tilade) inhibit the
antigen-antibody reaction on mast cells that
triggers allergic reactions
• Administration is by oral inhalation
• Drugs are used on a daily basis and are
intended to prevent or decrease allergic
reactions
• Several weeks are usually required for the full
therapeutic effect
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Mucolytics
• Mucolytics are intended to break apart and
liquefy thick respiratory secretions to
facilitate easier removal
• Acetylcysteine (Mucomist) is the most
widely used mucolytic and is inhaled by
nebulization
• Administration is usually followed by
postural drainage and tracheal suction
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