Lilley, Shelly Collins, Julie Snyder Chapter 1-58
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1. bronchodilators overview: Bronchodilators are an important part of the pharma-
cotherapy for all respiratory diseases. These drugs relax bronchial smooth muscle,
which causes dilation of the bronchi and bronchioles that are narrowed as a result
of the disease process. There are three classes of such drugs: beta adrenergic
agonists, anticholinergics, and xanthine derivatives.
2. beta andregenic drug overview: The beta-adrenergic agonists are a group of
drugs that are commonly used during the acute phase of an asthmatic attack to
quickly reduce airway constriction and restore airflow to normal. They are agonists
of the adrenergic receptors in the sympathetic nervous system. The beta and alpha
adrenergic receptors are discussed in Chapters 18 and 19. The beta agonists
imitate the effects of norepinephrine on beta receptors. For this reason, they are
also called sympathomimetic bronchodilators. The beta agonists are categorized by
their onset of action. Short-acting beta agonist (SABA) inhalers include albuterol
(Ventolin), levalbuterol (Xopenex), pirbuterol (Maxair), terbutaline (Brethine), and
metaproterenol (Alupent). Long-acting beta agonist (LABA) inhalers include arfor-
moterol (Brovana), formoterol (Foradil, Perforomist), and salmeterol (Serevent). The
newest long-acting beta agonists are indacterol (Arcapta Neohaler); vilanterol in
conjunction with fluticasone (Breo Ellipta); and vilanterol in conjunction with the
anticholinergic umeclidinium (Anoro Ellipta). The term Ellipta refers to a new delivery
system. Because the long-acting beta agonists (LABAs) have a longer onset of
action, they must never be used for acute treatment. Patients must be taught to use
the short-acting beta agonist (SABA) as rescue treatment.
3. short acting beta agonist: albuterol (Ventolin), levalbuterol (Xopenex), pirbuterol
(Maxair), terbutaline (Brethine), and metaproterenol (Alupent).
4. Albuterol: Class : beta 2 agonist (short acting)
Indications and mechanisms of action: is a short-acting beta2-specific bronchodi-
lating beta agonist. Other similar drugs include bitolterol (Tornalate), levalbuterol
(Xopenex), pirbuterol (Maxair), and terbutaline (Brethine). Albuterol is the most
commonly used drug in this class. If albuterol is used too frequently, dose-related
adverse effects may be seen, because albuterol loses its beta2-specific actions,
especially at larger dosages
Contraindications :. As a consequence, the beta1 receptors are stimulated, which
causes nausea, increased anxiety, palpitations, tremors, and an increased heart
rate.
, Test Bank for Pharmacology and the Nursing Process 10th Edition By Li
Lilley, Shelly Collins, Julie Snyder Chapter 1-58
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Route: po and inhalation
Other facts: levorotatory isomeric form of albuterol, levalbuterol, is sometimes pre-
scribed as an albuterol alternative for patients with certain risk factors (e.g., tachy-
cardia, including tachycardia associated with albuterol treatment). (Lilley 583)Lilley,
Linda, Shelly Collins, Julie Snyder. Pharmacology and the Nursing Process, 8th
Edition. Mosby, 022016. VitalBook file.
5. long acting beta agonist: arformoterol (Brovana), formoterol (Foradil, Per-
foromist), and salmeterol (Serevent). The newest long-acting beta agonists are in-
dacterol (Arcapta Neohaler); vilanterol in conjunction with fluticasone (Breo Ellipta);
and vilanterol in conjunction with the anticholinergic umeclidinium (Anoro Ellipta)
6. beta andregenic mechanism of action and drug effect: The beta agonists
relax and dilate airways by stimulating the beta2-adrenergic receptors located
throughout the lungs.
582
There are three subtypes of these drugs, based on their selectivity for beta2
receptors:
1. Nonselective adrenergic drugs, which stimulate the beta, beta1 (cardiac), and
beta2 (respiratory) receptors. Example: epinephrine. (NOTE: Epinephrine inhalers
were taken off the market in 2012 because they did not comply with FDA require-
ments). Epinephrine is available as a prefilled syringe for self-administration by
patients with severe allergic reactions and is called EpiPen (Figure 37-2).
2. Nonselective beta-adrenergic drugs, which stimulate both beta1 and beta2 recep-
tors. Example: metaproterenol.
3. Selective beta2 drugs, which primarily stimulate the beta2 receptors. Example:
albuterol.
These drugs can also be categorized according to their routes of administration as
oral, injectable, or inhaled. The various beta agonist bronchodilators are listed in
Table 37-3. The bronchioles are surrounded by smooth muscle. When the smooth
muscle contracts, the airways are narrowed and the amount of oxygen and carbon
dioxide exchanged is reduced. The action of beta agonist bronchodilators begins
at the specific receptor stimulated and ends with the relaxation and dilation of the
airways. However, many reactions must take place at the cellular level for bronchodi-
lation to occur. When a beta2-adrenergic receptor is stimulated by a beta agonist,
, Test Bank for Pharmacology and the Nursing Process 10th Edition By Li
Lilley, Shelly Collins, Julie Snyder Chapter 1-58
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adenylate cyclase is activated and produces cyclic adenosine monophosphate
(cAMP). Adenylate cyclase is an enzyme needed to make cAMP. The increased
levels of cAMP cause bronchial smooth muscles to relax, which results in bronchial
dilation and increased airflow into and out of the lungs.
Nonselective adrenergic agonist drugs such as epinephrine also stimulate alpha-ad
7. indications of beta andregenics: The primary therapeutic effect of the beta
agonists is the prevention or relief of bronchospasm related to bronchial asthma,
bronchitis, and other pulmonary diseases. However, they are also used for effects
outside the respiratory system. Because some of these drugs have the ability to
stimulate both beta1- and alpha-adrenergic receptors, they may be used to treat
hypotension and shock (see Chapter 18).
8. contraindications for beta andregenics: drug allergy, uncontrolled hyperten-
sion or cardiac dysrhythmias, and high risk for stroke (because of the vasoconstric-
tive drug action)
9. adverse effects of beta andregenics: Mixed alpha/beta agonists produce the
most adverse effects because they are nonselective. These include insomnia,
restlessness, anorexia, cardiac stimulation, hyperglycemia, tremor, and vascular
headache. The adverse effects of the nonselective beta agonists are limited to
beta-adrenergic effects, including cardiac stimulation, tremor, anginal pain, and
vascular headache. The beta2 drugs can cause both hypertension and hypotension,
vascular headaches, and tremor. Overdose management may include careful ad-
ministration of a beta blocker while the patient is under close observation due to the
risk for bronchospasm. Because the half-life of most adrenergic agonists is relatively
short, the patient may just be observed while the body eliminates the medication.
10. interactions with beta andregenics: When nonselective beta blockers are
used with the beta agonist bronchodilators, the bronchodilation from the beta ag-
onist is diminished. The use of beta agonists with monoamine oxidase inhibitors
and other sympathomimetics is best avoided because of the enhanced risk for
hypertension. Patients with diabetes may require an adjustment in the dosage of
their hypoglycemic drugs, especially patients receiving epinephrine, because of the
increase in blood glucose levels that can occur.
11. Salmeterol (Serevent Diskus) (Lilley 583): Class : long acting beta 2 agonist
is a long-acting beta2 agonist bronchodilator. Other long-acting inhalers include
formoterol (Foradil, Perforomist), arformoterol (Brovana), and indacterol (Arcapta
Neohaler). The long-acting inhalers are never to be used for acute treatment.
Salmeterol is used for the maintenance treatment of asthma and COPD and is used
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Lilley, Shelly Collins, Julie Snyder Chapter 1-58
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in conjunction with an inhaled corticosteroid. It is given twice daily for maintenance
treatment only. In 2006, a large randomized clinical trial showed that use of sal-
meterol was associated with an increase in asthma-related deaths (when added to
usual asthma therapy). The risk appears to be higher in African-American patients.
All LABAs have a black box warning regarding this risk. Adverse effects include
immediate hypersensitivity reactions, headache, hypertension, and neuromuscular
and skeletal pain. Salmeterol should never be given more than twice daily nor
should the maximum daily dose (one puff twice daily) be exceeded. It is available
as a powder for inhalation either alone (Serevent Diskus) or combined with a
corticosteroid (Advair). The long-acting inhalers, including salmeterol, are not to be
used alone, but in combination with other drugs such as the inhaled corticosteroids.
Advair (salmeterol and fluticasone) is a very popular inhaler for COPD. Symbicort,
a newer inhaler consisting of the corticosteroid budesonide and the bronchodilator
formoterol, is similar to Advair as is Dulera, which is a combination of formoterol and
mometasone. (Lilley 583)Lilley, Linda, Shelly Collins, Julie Snyder. Pharmacology
and the Nursing Process, 8th Edition. Mosby, 022016. VitalBook file.
12. Anti cholinergics mechanism of action and drug affects: On the surface of
the bronchial tree are receptors for acetylcholine (ACh), the neurotransmitter for the
parasympathetic nervous system (PSNS). When the PSNS releases ACh from its
nerve endings, it binds to the ACh receptors on the surface of the bronchial tree,
which results in bronchial constriction and narrowing of the airways. Anticholinergic
drugs block these ACh receptors to prevent bronchoconstriction. This indirectly
causes airway relaxation and dilation. Anticholinergic agents also help reduce
secretions in COPD patients. (Lilley 584)Lilley, Linda, Shelly Collins, Julie Snyder.
Pharmacology and the Nursing Process, 8th Edition. Mosby, 022016. VitalBook file.
13. Indications of anti cholinergics: Because their actions are slow and pro-
longed, anticholinergics are used for the prevention of bronchospasm associated
with chronic bronchitis or emphysema and not for the management of acute symp-
toms. (Lilley 584)Lilley, Linda, Shelly Collins, Julie Snyder. Pharmacology and the
Nursing Process, 8th Edition. Mosby, 022016. VitalBook file.
14. Contraindications to anticholinergics: The only usual contraindication to the
use of bronchial anticholinergic drugs is known drug allergy, including allergy to
atropine. In the past, an allergy to peanuts or soy was listed as a contraindication
to ipratropium inhalers. This was related to the propellant used, and the new HFA
inhalers have eliminated the concern. Thus, there is no contraindication using iprat-
ropium in patients with peanut or soy allergies. Caution is necessary in patients with
acute narrow-angle glaucoma and prostate enlargement (Lilley 584)Lilley, Linda,
Shelly Collins, Julie Snyder. Pharmacology and the Nursing Process, 8th Edition.
Mosby, 022016. VitalBook file.