Shelly Collins, Julie Snyder Chapter 1-58
1. bronchodilators overview: Bronchodilators are an important part of the pharmacotherapy 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 arformoterol (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 bronchodilating 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.
Route: po and inhalation
Other facts: levorotatory isomeric form of albuterol, levalbuterol, is sometimes prescribed as an albuterol alternative for patients with
certain risk factors (e.g., tachycardia, 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, 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) 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:
, Test Bank for Pharmacology and the Nursing Process 10th Edition By Lind Lilley,
Shelly Collins, Julie Snyder Chapter 1-58
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 requirements).
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 receptors. 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 bronchodilation to occur. When a beta2-adrenergic receptor is stimulated by a beta agonist, 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 hypertension or cardiac dysrhythmias, and high risk for
stroke (because of the vasoconstrictive 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 administration 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 agonist 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
, Test Bank for Pharmacology and the Nursing Process 10th Edition By Lind Lilley,
Shelly Collins, Julie Snyder Chapter 1-58
and is used 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 salmeterol 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 prolonged, anticholinergics are used for the prevention of bronchospasm associated with chronic bronchitis or
emphysema and not for the management of acute symptoms. (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 ipratropium 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.
15. Adverse effects to anticholinergics: The most commonly reported adverse effects of inhaled anticholinergics are related to
their pharmacology and include dry mouth or throat, nasal congestion, heart palpitations, gastrointestinal (GI) distress, urinary
retention, increased intraocular pressure, headache, coughing, and anxiety. Ipratropium is classified as a pregnancy category B
drug; all others in this class are pregnancy category C.
(Lilley 584) Lilley, Linda, Shelly Collins, Julie Snyder. Pharmacology and the Nursing Process, 8th Edition. Mosby, 022016. VitalBook file.
16. Drug interactions anticholinergics: Possible additive toxicity may occur when anticholinergic bronchodilators are taken with
other anticholinergic drugs.
(Lilley 584) Lilley, Linda, Shelly Collins, Julie Snyder. Pharmacology and the Nursing Process, 8th Edition. Mosby, 022016. VitalBook file.
, Test Bank for Pharmacology and the Nursing Process 10th Edition By Lind Lilley,
Shelly Collins, Julie Snyder Chapter 1-58
17. Ipratropium (Atrovent): Class : anticholinergic
Indications and mechanisms of action : is the oldest anticholinergic bronchodilator. It is pharmacologically very similar to atropine (see
Chapter 21). It is available both as a liquid aerosol for inhalation and as a multidose inhaler; both forms are usually dosed twice daily.
Tiotropium (Spiriva) and aclidinium (Tudorza) are similar drugs. Spiriva is given once a day, whereas Tudorza is given twice daily. Many
patients also benefit from taking both a beta2 agonist and an anticholinergic drug, with the most popular combination being albuterol
and ipratropium. Although many patients receive the two drugs separately, two combination products are available containing both of
these drugs: Combivent (an MDI) and DuoNeb (an inhalation solution). (Lilley 584) Route : inhaler
18. Xanthine Derivatives overview: The natural xanthines consist of the plant alkaloids caffeine, theobromine, and theophylline,
but only theophylline and caffeine are currently used clinically. Synthetic xanthines include aminophylline and dyphylline. Caffeine
which is actually a metabolite of theophylline, has other uses described later in the chapter. (Lilley 584) Lilley, Linda, Shelly Collins,
Julie Snyder. Pharmacology and the Nursing Process, 8th Edition. Mosby, 022016. VitalBook file. 19. Xanthine mechanism of
action: Xanthines cause bronchodilation by increasing the levels of the energy-producing substance cAMP. They do this by
competitively inhibiting phosphodiesterase, the enzyme responsible for breaking down cAMP. In patients with COPD, cAMP plays
an integral role in the maintenance of open airways. Higher intracellular levels of cAMP contribute to smooth muscle relaxation
and also inhibit IgE-induced release of the chemical mediators that drive allergic reactions (histamine, slow-reacting substance of
anaphylaxis, and others).
Theophylline is metabolized to caffeine in the body, whereas aminophylline is metabolized to theophylline. Theophylline and other
xanthines stimulate the CNS, but to a lesser degree than caffeine. This stimulation of the CNS has the beneficial effect of acting directly o
the medullary respiratory center to enhance respiratory drive. In large doses, theophylline may stimulate the cardiovascular system, whi
results in both an increased force of contraction (positive inotropy) and an increased heart rate (positive chronotropy). The increased
force of contraction raises cardiac output and hence blood flow to the kidneys. This, in combination with the ability of the xanthines to
dilate blood vessels in and around the kidney, increases the glomerular filtration rate, which produces a diuretic effect. (Lilley 584) Lilley
Linda, Shelly Collins, Julie Snyder. Pharmacology and the Nursing Process, 8th Edition. Mosby, 022016.
VitalBook file.
20. Xanthine Indications: Xanthines are used to dilate the airways in patients with asthma, chronic bronchitis, or emphysema.
They may be used in mild to moderate cases of acute asthma and as an adjunct drug in the management of COPD. Xanthines are now
deemphasized because of their potential for drug interactions and the interpatient variability in therapeutic drug levels in the blood.
Because of their relatively slow onset of action, xanthines are used for the prevention of asthmatic symptoms and COPD, not for the
relief of acute asthma attacks.
Caffeine is used without prescription as a CNS stimulant, or analeptic (see Chapter 13), to promote alertness (e.g., for long-duration
driving or studying). It is also used as a cardiac stimulant in infants with bradycardia and for enhancement of respiratory drive in infants.
(Lilley 585) Lilley, Linda, Shelly Collins, Julie Snyder. Pharmacology and the Nursing Process, 8th Edition. Mosby, 022016. VitalBook file.
21. Xanthine contraindications: Contraindications to therapy with xanthine derivatives include known drug allergy, uncontrolle
cardiac dysrhythmias, seizure disorders, hyperthyroidism, and peptic ulcers. (Lilley 585) Lilley, Linda, Shelly Collins, Julie Snyder.
Pharmacology and the Nursing Process, 8th Edition. Mosby, 022016.