Bronchodilators and Other

Respiratory Drugs
 Asthma

 Emphysema

 Chronic bronchitis
 Recurrent and reversible shortness of breath
 Airways become narrow as a result of:
• Bronchospasm
• Inflammation & Edema of the bronchial mucosa
• Production of viscid mucus

 Alveolar ducts/alveoli remain open, but airflow to them is obstructed

 Symptoms
• Wheezing
• Difficulty breathing
 Status asthmaticus

• Prolonged asthma attack that does not respond to

typical drug therapy
• May last several minutes to hours
• Medical emergency
 Continuous inflammation of the bronchi and
bronchioles

 Often occurs as a result of prolonged exposure

to bronchial irritants

 Characterized by
• Hypoxemia
• Chronic productive cough
• “Blue Bloater”
 Air spaces enlarge as a result of the destruction
of alveolar walls
 The surface area where gas exchange takes place
is reduced
 Effective respiration is impaired
 Characterized by:
• Increased paCO2 - respiratory acidosis
• Difficulty exhaling – pursed lip breathing
• “Pink Puffer”
 Long-term control
• Antileukotrienes
• cromolyn
• Inhaled steroids
• Long-acting β2-agonists

 Quick relief
• Intravenous systemic corticosteroids
• Short-acting inhaled β2-agonists
 Bronchodilators
• β-adrenergic agonists
• Xanthine derivatives

 Anticholinergics

 Antileukotrienes

 Corticosteroids
 Large group, sympathomimetics

 Used during acute phase of asthmatic attacks

 Quickly reduce airway constriction

 Stimulate β2-adrenergic receptors throughout

the lungs
Three types
 Nonselective adrenergics
• Stimulate α, β1 (cardiac), and β2 (respiratory) receptors
• Example: epinephrine
 Nonselective β-adrenergics
• Stimulate both β1 and β2 receptors
• Example: metaproterenol

 Selective β2 drugs
• Stimulate only β2 receptors
•
 Mechanism of Action

 Begins at the specific receptor stimulated#

 Ends with the dilation of the airways

• #Activation of β2 receptors activates cAMP,* which

relaxes smooth muscles of the airway and results in
bronchial dilation and increased airflow
*cAMP = cyclic adenosine monophosphate
 Indications
 Relief of bronchospasm related to asthma, bronchitis, and other
pulmonary diseases
 Useful in treatment of acute attacks as well as prevention
 Used in hypotension and shock
 Used to produce uterine relaxation to prevent premature labor
 Hyperkalemia—stimulates potassium to shift into the cell
α-β (epinephrine)

 Insomnia  Hyperglycemia
 Restlessness  Tremor
 Anorexia  Cardiac stimulation
 Vascular headache
β1 and β2 (metaproterenol)
 Cardiac stimulation 
Vascular headache
 Tremor  Hypotension
 Anginal pain
β2 (albuterol)
 Hypotension OR hypertension
 Vascular headache
 Tremor
 Thorough assessment before beginning therapy

• Skin color
• Baseline vital signs
• Respirations (should be between 12 and 24 breaths/min)
• Respiratory assessment, including PO2
• Sputum production
• Allergies
• History of respiratory problems
• Other medications
 Monitor for therapeutic effects
• Decreased dyspnea
• Decreased wheezing, restlessness, and anxiety
• Improved respiratory patterns with return to normal rate and
quality
• Improved activity tolerance

 Patients should know how to use inhalers and MDIs

• Have patients demonstrate use of devices

 Monitor for adverse effects

 Patients should be encouraged to have a good state of health

• Avoid exposure to conditions that precipitate bronchospasms (allergens,

smoking, stress, air pollutants)
• Adequate fluid intake
• Compliance with medical treatment
• Avoid excessive fatigue, heat, extremes in temperature, caffeine

 Patients to get prompt treatment for flu or other illnesses

 Patients to get vaccinated against pneumonia and flu

 Check with their physician before taking any medication, including OTCs

 Teach patients to take bronchodilators exactly as prescribed

 Albuterol, if used too frequently, loses its β2-specific actions at
larger doses
• As a result, β1 receptors are stimulated, causing nausea, increased
anxiety, palpitations, tremors, and increased heart rate

 Take medications exactly as prescribed

• No omissions or double doses

 Report insomnia, jitteriness, restlessness, palpitations, chest

pain, or any change in symptoms
 For any inhaler prescribed, ensure that the patient is able to
self-administer the medication

• Provide demonstration and return demonstration

• Ensure the patient knows the correct time intervals for

inhalers

• Provide a spacer if the patient has difficulty coordinating

breathing with inhaler activation

• Ensure that patient knows how to keep track of the

number of doses in the inhaler device
 Mechanism of Action
 Acetylcholine (ACh) causes bronchial constriction and narrowing of
the airways
 Anticholinergics bind to the ACh receptors, preventing ACh from
binding

 Result:
• bronchoconstriction is prevented
• airways dilate

 ipratropium bromide (Atrovent) and tiotropium (Spiriva)

 Slow and prolonged action
 Used to prevent bronchoconstriction
 NOT used for acute asthma exacerbations!
 Adverse effects
 Dry mouth or throat
 Nasal congestion
 Heart palpitations
 Gastrointestinal distress
 Headache
 Coughing
 Anxiety

No known drug interactions

 Plant alkaloids:
• caffeine, theobromine, and theophylline

 Only theophylline is used as a bronchodilator

 Synthetic xanthines:
(IV) theophylline (Aminophylline)
(oral) theophylline (Elixophyllin, Theo-Dur)
 Increase levels of energy-producing cAMP
• This is done competitively inhibiting phosphodiesterase
(PDE), the enzyme that breaks down cAMP (cAMP = cyclic
adenosine monophosphate)

 Result:
• decreased cAMP levels, smooth muscle relaxation, bronchodilation, and
increased airflow
• cardiovascular stimulation: increased force of contraction and increased
heart rate, resulting in increased cardiac output and increased blood flow to the
kidneys (diuretic effect)
 Dilate of airways in asthma, chronic bronchitis, and emphysema

 Mild to moderate cases of acute asthma

 Adjunct drug in the management of COPD

 Not used as frequently due to:

• potential for drug interactions
• variables related to drug levels in the blood
 Nausea, vomiting, anorexia

 Gastroesophageal reflux during sleep

 Sinus tachycardia, extrasystoles, palpitations,

ventricular dysrhythmias

 Transient increased urination

 Contraindications: history of PUD or GI disorders
 Cautious use: cardiac disease
 Timed-release preparations should not be crushed or chewed
(causes gastric irritation)
 Report to physician:
• Palpitations Nausea Vomiting
• Weakness Dizziness Chest pain
• Convulsions
 Interactions with cimetidine, oral contraceptives, allopurinol,
certain antibiotics elevate serum xanthine blood levels
 Nicotine & caffeine potentiate cardiac effects
 St. John’s wort increases metabolism = decrease blood levels
 Also called
leukotriene receptor antagonists (LRTAs)

 Newer class of asthma drugs

Currently available drugs

 montelukast (Singulair)
 zafirlukast (Accolate)
 zileuton (Zyflo)
 Leukotrienes

• substances released when a trigger, such as cat hair or

dust, starts a series of chemical reactions in the body
• cause inflammation, bronchoconstriction, and mucus
production

 Result: coughing, wheezing, shortness of breath

 Antileukotriene drugs
• prevent leukotrienes from attaching to receptors on cells in and in circulation
 Inflammation in the lungs is blocked
 Asthma symptoms are relieved

By blocking leukotrienes:
 Prevent smooth muscle contraction of the bronchial airways
 Decrease mucus secretion
 Prevent vascular permeability
 Decrease neutrophil and leukocyte infiltration to the lungs,

preventing inflammation
 Prophylaxis and chronic treatment of asthma in
adults and children older than
age 12
 NOT meant for management of acute asthmatic
attacks
 montelukast (Singulair)
• is approved for use in children ages 2 and older, and for
treatment of allergic rhinitis
zileuton (Zyflo) zafirlukast (Accolate)

Headache Headache
Dyspepsia Nausea
Nausea Diarrhea
Dizziness Liver dysfunction
Insomnia
Liver dysfunction

Montelukast (Singulair) has fewer adverse effects

 Ensure that the drug is being used for chronic management of asthma,
not acute asthma

 Teach the patient the purpose of the therapy

 Improvement should be seen in about 1 week

 Check with physician before taking any OTC or prescribed medications—

many drug interactions
 Assess liver function before beginning therapy
 Medications should be taken every night on a continuous schedule,
even if symptoms improve
 Anti-inflammatory!!!
 Uses - chronic asthma/COPD exacerbations
 Do not relieve acute asthmatic attacks S&S
 Oral, IV (quick acting), or inhaled forms
 Inhaled forms reduce systemic effects
• May take several weeks before full
effects are seen
 Mechanism of Action
 Stabilize membranes of cells that release
harmful bronchoconstricting substances

 Also increase responsiveness of bronchial

smooth muscle to β-adrenergic stimulation
 beclomethasone dipropionate
(Beclovent, Vanceril)

 triamcinolone acetonide (Azmacort)

 dexamethasone sodium phosphate (Decadron

Phosphate Respihaler)

 fluticasone (Flovent, Flonase)

 Treatment of bronchospastic disorders
that are not controlled by conventional
bronchodilators

 NOT considered first-line drugs for management

of acute asthmatic attacks
or status asthmaticus
 Pharyngeal irritation

 Coughing

 Dry mouth

 Oral fungal infections

 Systemic effects are rare because of the low

doses used for inhalation therapy
 Contraindicated in patients with psychosis, fungal infections,
AIDS, TB

 Teach patients to gargle and rinse the mouth with lukewarm

water afterward to prevent the development of oral fungal
infections

 If a β-agonist bronchodilator and corticosteroid inhaler are both

ordered, the bronchodilator should be used several minutes
before the corticosteroid to provide bronchodilation before
administration of the corticosteroid
 Teach patients
• to monitor disease with a peak flow meter

• use of a spacer device to ensure successful

inhalations

• keep inhalers and nebulizer equipment clean after

uses

• Tapering doses of oral corticosteroids

1. Doses of xanthine derivatives may need to be reduced in older adult patients. True or false?
Explain your answer.

2. The therapeutic blood level of theophylline in the adult is _____________

3. Theophylline is classified as a _____________ _____________, whereas albuterol

(Proventil) and epinephrine (Medinhaler-Epi) are _____________________
______________.

4. β-agonists are contraindicated in patients with _________ or _________ disorders.

5. Antileukotriene drugs reduce _______________ associated with asthma, and are used for
chronic/acute asthma.

6. This antileukotriene drug is US Food and Drug Administration (FDA) approved for use in
children 2 years of age and older: ___________________.
1. Lower doses in the older adult may be necessary initially and during therapy with close monitoring
for adverse effects and toxicity (cardiovascular and central nervous system [CNS] stimulation).

2. The therapeutic blood level of theophylline in the adult is 10 to 20 mcg/mL; some practitioners
recommend 5 to 15 mcg/mL

3. Theophylline is classified as a xanthine derivative, whereas albuterol and epinephrine are β-agonist
bronchodilators.

4. β-agonists are contraindicated in patients with a high risk of stroke or any cardiovascular disorders,
particularly tachydysrhythmias.

5. Antileukotriene drugs reduce inflammation associated with asthma, and are used for chronic
asthma.

6. This antileukotriene drug is US Food and Drug Administration (FDA) approved for use in children
2 years of age and older: montelukast (Singulair).
 For each drug listed, state whether it is used for:

 A. Asthma prophylaxis and maintenance treatment

 B. Treatment of acute bronchospasm
 C. Both

1. montelukast (Singulair), an antileukotriene

2. theophylline (Theo-Dur) oral tablets, xanthine-derived

3. fluticasone (Flovent), a synthetic glucocorticoid

4. ipratropium (Atrovent), an anticholinergic

5. albuterol Proventil) inhaler, a β 1 agonist

6. epinephrine, intravenous dose, an alpha-beta agonist

1. A

2. A (not used as much now for relief of acute symptoms, especially

the oral form)

3. A

4. C

5. C

6. B (for the IV form)