Bronchodilators & Beta Adrenergic Agonists

Beta-adrenergic Agonists (or beta agonists)

The first-line drugs for the treatment of acute asthma

Activates the Sympathetic Nervous System
o Relaxes bronchial smooth muscle
Bronchodilation
Easier breathing for patient
Can act on both beta1 and beta2 receptors
o Beta1 located in heart
o Beta2 located in smooth muscle of lungs, uterus, and other organs
o Acting on both = nonselective drugs
Ex: epinephrine and isoproterenol (Isuprel)
o Acting solely on beta2 has replaced the use of nonselective drugs and
these are called selective drugs, respectively
Produce fewer cardiac side effects
No anti-inflammatory properties
o Must be used in conjunction with other drug classes in treatment of
chronic asthma
Three classes of beta-agonists by duration
o Short-acting
Pirbuterol (Maxair)
Rapid onset of action-usually several minutes
Most frequently prescribed for aborting or terminating an acute
asthma attach
Rescue Drugs
Effects only last 2-6 hours
Limits use to as needed, PRN, for acute episodes
o Moderate-acting
Therapeutic effects last about 8 hours
o Long-acting beta agonists (LABA)
Last up to 12 hours
Have slow onset of action
Delivered via inhalers just like short-acting drugs
In 2005 FDA issued a black box warning regarding an increase in
deaths
Taking LABA to abort an asthma attack can result in
unrelieved bronchospasm and subsequent death
o Patients must be alerted to the risk of taking LABAs
for an acute episode
Should only be used as adjunctive therapy
For patients who cannot be adequately controlled with
other medications such as inhaled corticosteroids

For patients with severe asthma who clearly require two

medications
Should not be used as mono-therapy
Available forms
o PO
Longer duration
Increase in systemic adverse reactions
Could activate beta1 receptors in the heart
o Angina attack
o Dysrhythmia
o Inhaled
Most common route for respiratory conditions
Minimal systemic toxicity because only small amounts of the
drug are absorbed
o Parenteral formulations
Chronic use can lead to tolerance
o Duration of action could become shorter
o Doses may need to be increased
o Different drugs may need to be added to regimen
Increased use of beta agonist over a period of hours or days:
o Indication that the patients condition is rapidly deteriorating
o Medical attention should be sought immediately
Drugs in this category:
o albuterol
Proventil, Ventolin, and Vospire
o arformoterol
Brovana
o formoterol
Foradil, Perforomist
o indacaterol
Arcapta neohaler
o metaproterenol
o pirbuterol
Maxair
o salmeterol
Serevent
o terbutaline
Brethine

Anticholinergics (aka cholinergic blockers/antagonists)

These are alternative bronchodilators for patients unable to tolerate beta 2

adrenergic agonists
Block parasympathetic nervous system
Results in effects similar to stimulating the sympathetic system
Administered via inhalation has least adverse effects (MDI)
Oral & parenteral routes (of atropine i.e.) cause too many adverse effects
Three drugs:

1. ipratropium (Atrovent)
Most commonly prescribed anticholinergic for COPD & asthma
Slower onset of action than beta agonists
Produces less bronchodilation
When combined w/ a beta agonist, together they produce greater and
more prolonged bronchodilation than either one separately
2. tiotropium (Spiriva)
Longer duration of action, for long-term maintenance
treatment/prophylaxis of bronchospasm for COPD, chronic
bronchitis, & emphysema
3. aclidimium (Tudorza Pressair)
These are relatively safe drugs-only small amount absorbed into lungs
Rarely produce systemic adverse effects
Mild side effects include:
o Dry mouth
o GI distress
o Headache
o Anxiety
o Bitter taste, rinse mouth after use
Contraindications
Patients with sensitivity to soya lecithin, soy or peanuts (soy lecithin uses
as propellant)
Interactions
Use w/other drugs in this class can lead to additive anticholinergic side
effects

Methylxanthines
Mainly used for long term management of persistent asthma that does not
respond to beta agonists or
inhaled corticosteroids
Administered PO or IV routs instead of inhalation
There are two types of methylxanthines which are bronchodilators chemically
related to caffeine.
Theophylline (Theo-Dur, others)
Aminophylline (Truphylline)
Are rarely prescribed due to their narrow safety margin particularly with continued
use
Common Adverse Effects:
Nervousness & Insomnia (similar to effects caffeine causes)
Tremors
Dizziness
Headache
Nausea
Vomiting
Anorexia
Serious Adverse Effects

CNS stimulation
Seizures
Hypotension
High doses can result in:
o Dysrhythmias = abnormal beating of the heart
o Tachycardias = beating too fast
o Bradycardia = beating too slow
Circulatory failure
Respiratory arrest
Significant interactions with many other drugs

Questions
1. A patient is experiencing an acute asthma attack. What is the first-line therapy
for relief of an acute asthma attack?
a) Beta2-adrenergic agonist
b) Methylxanthines
c) Anticholinergics
2. A patient is instructed on the administration of inhaled corticosteroid agents to
treat asthma. How do inhaled corticosteroid agents assist in the treatment of
asthma?
a) Inhaled corticosteroid agents will activate the parasympathetic nervous
system
b) Inhaled corticosteroid agents will reduce respiratory rate
c) Inhaled corticosteroid agents will reduce bronchodilation
d) Inhaled corticosteroid agents will reduce airway inflammation