A bronchodilator or broncholytic (although the latter occasionally includes
secretory inhibition as well) is a substance that dilates the
bronchi
A bronchus is a passage or airway in the lower respiratory tract that conducts air into the lungs. The first or primary bronchi pronounced (BRAN-KAI) to branch from the trachea at the carina are the right main bronchus and the left main bronchus. ...
and
bronchiole
The bronchioles or bronchioli (pronounced ''bron-kee-oh-lee'') are the smaller branches of the bronchial airways in the lower respiratory tract. They include the terminal bronchioles, and finally the respiratory bronchioles that mark the start ...
s, decreasing resistance in the
respiratory airway and increasing airflow to the
lungs. Bronchodilators may be
originating naturally within the body, or they may be
medication
A medication (also called medicament, medicine, pharmaceutical drug, medicinal drug or simply drug) is a drug used to diagnose, cure, treat, or prevent disease. Drug therapy ( pharmacotherapy) is an important part of the medical field and ...
s administered for the treatment of breathing difficulties, usually in the form of
inhaler
An inhaler (also known as a puffer, pump or allergy spray) is a medical device used for delivering medicines into the lungs through the work of a person's breathing. This allows medicines to be delivered to and absorbed in the lungs, which prov ...
s. They are most useful in
obstructive lung disease
Obstructive lung disease is a category of respiratory disease characterized by airway obstruction. Many obstructive diseases of the lung result from narrowing (obstruction) of the smaller bronchi and larger bronchioles, often because of excessiv ...
s, of which
asthma
Asthma is a long-term inflammatory disease of the airways of the lungs. It is characterized by variable and recurring symptoms, reversible airflow obstruction, and easily triggered bronchospasms. Symptoms include episodes of wheezing, co ...
and
chronic obstructive pulmonary disease
Chronic obstructive pulmonary disease (COPD) is a type of progressive lung disease characterized by long-term respiratory symptoms and airflow limitation. The main symptoms include shortness of breath and a cough, which may or may not produce ...
are the most common conditions. Although this remains somewhat controversial, they might be useful in
bronchiolitis
Bronchiolitis is inflammation of the small airways in the lungs. Acute bronchiolitis is due to a viral infection usually affecting children younger than two years of age. Symptoms may include fever, cough, runny nose, wheezing, and breathing ...
and
bronchiectasis. They are often prescribed but of unproven significance in
restrictive lung disease
Restrictive lung diseases are a category of extrapulmonary, pleural, or parenchymal respiratory diseases that restrict lung expansion, resulting in a decreased lung volume, an increased work of breathing, and inadequate ventilation and/or oxygenat ...
s.
Bronchodilators are either short-acting or long-acting. Short-acting medications provide quick or "rescue" relief from acute
bronchoconstriction
Bronchoconstriction is the constriction of the airways in the lungs due to the tightening of surrounding smooth muscle, with consequent coughing, wheezing, and shortness of breath.
Causes
The condition has a number of causes, the most common be ...
. Long-acting bronchodilators help to control and prevent symptoms. The three types of prescription bronchodilating drugs are
beta2-adrenergic agonist
Beta2-adrenergic agonists, also known as adrenergic β2 receptor agonists, are a class of drugs that act on the β2 adrenergic receptor. Like other β adrenergic agonists, they cause smooth muscle relaxation. β2 adrenergic agonists' effect ...
s (short- and long-acting),
anticholinergics
Anticholinergics (anticholinergic agents) are substances that block the action of the neurotransmitter called acetylcholine (ACh) at synapses in the central and peripheral nervous system.
These agents inhibit the parasympathetic nervous sy ...
(short- and long-acting), and
theophylline
Theophylline, also known as 1,3-dimethylxanthine, is a phosphodiesterase inhibiting drug used in therapy for respiratory diseases such as chronic obstructive pulmonary disease (COPD) and asthma under a variety of brand names. As a member of the ...
(long-acting).
Short-acting β2-adrenergic agonists
These are quick-relief or "rescue" medications that provide quick, temporary relief from asthma symptoms or flare-ups. These medications usually take effect within 20 minutes or less, and can last from four to six hours. These inhaled medications are best for treating sudden and severe or new asthma symptoms. Taken 15 to 20 minutes ahead of time, these medications can also prevent asthma symptoms triggered by exercise or exposure to cold air. Some short-acting β-agonists, such as
salbutamol, are specific to the lungs; they are called β
2-adrenergic agonists and can relieve bronchospasms without unwanted
cardiac
The heart is a muscular organ in most animals. This organ pumps blood through the blood vessels of the circulatory system. The pumped blood carries oxygen and nutrients to the body, while carrying metabolic waste such as carbon dioxide to t ...
side effects of nonspecific β-agonists (for example,
ephedrine
Ephedrine is a central nervous system (CNS) stimulant that is often used to prevent low blood pressure during anesthesia. It has also been used for asthma, narcolepsy, and obesity but is not the preferred treatment. It is of unclear benefit in ...
or
epinephrine). Patients who regularly or frequently need to take a short-acting β
2-adrenergic agonist should consult their doctor, as such usage indicates uncontrolled asthma, and their routine medications may need adjustment.
Long-acting β2-adrenergic agonists
These are long-term medications taken routinely in order to control and prevent bronchoconstriction. They are not intended for fast relief. These medications may take longer to begin working, but relieve airway constriction for up to 12 hours.
Commonly taken twice a day with an anti-inflammatory medication, they maintain open airways and prevent asthma symptoms, particularly at night.
Salmeterol
Salmeterol (sold in China as Qitai) is a long-acting β2 adrenergic receptor agonist (LABA) used in the maintenance and prevention of asthma symptoms and maintenance of chronic obstructive pulmonary disease (COPD) symptoms. Symptoms of bronchos ...
and
formoterol
Formoterol, also known as eformoterol, is a long-acting β2 agonist (LABA) used as a bronchodilator in the management of asthma and chronic obstructive pulmonary disease (COPD). Formoterol has an extended duration of action (up to 12 h) co ...
are examples of these.
Anticholinergics
Some examples of anticholinergics are
tiotropium
Tiotropium bromide, sold under the brand name Spiriva among others, is a long-acting bronchodilator (LAMA: long acting muscarinic antagonist) used in the management of chronic obstructive pulmonary disease (COPD) and asthma. Specifically it is ...
(Spiriva) and
ipratropium bromide.
Tiotropium is a long-acting, 24-hour, anticholinergic bronchodilator used in the management of
chronic obstructive pulmonary disease
Chronic obstructive pulmonary disease (COPD) is a type of progressive lung disease characterized by long-term respiratory symptoms and airflow limitation. The main symptoms include shortness of breath and a cough, which may or may not produce ...
(COPD).
Only available as an inhalant, ipratropium bromide is used in the treatment of asthma and COPD. As a short-acting anticholinergic, it improves lung function and reduces the risk of exacerbation in people with symptomatic asthma. However, it will not stop an asthma attack already in progress. Because it has no effect on asthma symptoms when used alone, it is most often paired with a short-acting β
2-adrenergic agonist. While it is considered a relief or rescue medication, it can take a full hour to begin working. For this reason, it plays a secondary role in acute asthma treatment. Dry throat is the most common side effect. If the medication gets in contact with the eyes, it may cause blurred vision for a brief time.
The use of anticholinergics in combination with short-acting β
2-adrenergic agonists has been shown to reduce hospital admissions in children and adults with acute asthma exacerbations.
Other
Available in oral and injectable form,
theophylline
Theophylline, also known as 1,3-dimethylxanthine, is a phosphodiesterase inhibiting drug used in therapy for respiratory diseases such as chronic obstructive pulmonary disease (COPD) and asthma under a variety of brand names. As a member of the ...
is a long-acting bronchodilator that prevents asthma episodes. It belongs to the chemical class
methylxanthine
Xanthine ( or ; archaically xanthic acid; systematic name 3,7-dihydropurine-2,6-dione) is a purine base found in most human body tissues and fluids, as well as in other organisms. Several stimulants are derived from xanthine, including caffeine, ...
s (along with caffeine). It is prescribed in severe cases of asthma or those that are difficult to control. It must be taken 1–4 times daily, and doses cannot be missed. Blood tests are required to monitor therapy and to indicate when dosage adjustment is necessary. Side effects can include nausea, vomiting, diarrhea, stomach or headache, rapid or irregular heart beat, muscle cramps, nervous or jittery feelings, and hyperactivity. These symptoms may signal the need for an adjustment in medication. It may promote
acid reflux
Gastroesophageal reflux disease (GERD) or gastro-oesophageal reflux disease (GORD) is one of the upper gastrointestinal chronic diseases where stomach content persistently and regularly flows up into the esophagus, resulting in symptoms and/ ...
, also known as GERD, by relaxing the lower esophageal sphincter muscle. Some medications, such as seizure and ulcer medications and antibiotics containing
erythromycin, can interfere with the way theophylline works. Coffee, tea, colas, cigarette-smoking, and viral illnesses can all affect the action of theophylline and change its effectiveness. A physician should monitor dosage levels to meet each patient's profile and needs.
Additionally some
psychostimulant drugs that have an amphetamine like mode of action, such as
amphetamine,
methamphetamine, and
cocaine
Cocaine (from , from , ultimately from Quechua: ''kúka'') is a central nervous system (CNS) stimulant mainly used recreationally for its euphoric effects. It is primarily obtained from the leaves of two Coca species native to South Ameri ...
, have bronchodilating effects and were used often for
asthma
Asthma is a long-term inflammatory disease of the airways of the lungs. It is characterized by variable and recurring symptoms, reversible airflow obstruction, and easily triggered bronchospasms. Symptoms include episodes of wheezing, co ...
due to the lack of effective β
2-adrenergic agonists for use as bronchodilator, but are now rarely, if ever, used medically for their bronchodilatory effects.
Common bronchodilators
The bronchodilators are divided into short- and long-acting groups. Short-acting bronchodilators are used for relief of bronchoconstriction, while long-acting bronchodilators are predominantly used for prevention.
Short-acting bronchodilators include:
*
Salbutamol/albuterol (Proventil or Ventolin)
*
Levosalbutamol/levalbuterol (Xopenex)
*
Pirbuterol
Pirbuterol (trade name Maxair) is a short-acting β2 adrenoreceptor agonist with bronchodilating action used in the treatment of asthma, available (as pirbuterol acetate) as a breath-activated metered-dose inhaler.
It was patented in 1971 a ...
(Maxair)
*
Epinephrine (Primatene Mist)
*
Racemic Epinephrine (Asthmanefrin, Primatene Mist Replacement)
*
Ephedrine
Ephedrine is a central nervous system (CNS) stimulant that is often used to prevent low blood pressure during anesthesia. It has also been used for asthma, narcolepsy, and obesity but is not the preferred treatment. It is of unclear benefit in ...
(Bronkaid)
*
Terbutaline
Terbutaline, sold under the brand names Bricanyl and Marex among others, is a β2 adrenergic receptor agonist, used as a "reliever" inhaler in the management of asthma symptoms and as a tocolytic (anti-contraction medication) to delay preterm ...
Long-acting bronchodilators include
*
Salmeterol
Salmeterol (sold in China as Qitai) is a long-acting β2 adrenergic receptor agonist (LABA) used in the maintenance and prevention of asthma symptoms and maintenance of chronic obstructive pulmonary disease (COPD) symptoms. Symptoms of bronchos ...
(Serevent or Seretide)
*
Clenbuterol
Clenbuterol is a sympathomimetic amine used by sufferers of breathing disorders as a decongestant and bronchodilator. People with chronic breathing disorders such as asthma use this as a bronchodilator to make breathing easier. It is most commonl ...
(Spiropent)
*
Formoterol
Formoterol, also known as eformoterol, is a long-acting β2 agonist (LABA) used as a bronchodilator in the management of asthma and chronic obstructive pulmonary disease (COPD). Formoterol has an extended duration of action (up to 12 h) co ...
*
Bambuterol
*
Indacaterol
Indacaterol is an ultra-long-acting beta-adrenoceptor agonist developed by Novartis. It needs to be taken only once a day, unlike the related drugs formoterol and salmeterol. It is licensed only for the treatment of chronic obstructive pulmonary d ...
Experimental bronchodilator
From among 6000 compounds that relax the smooth muscle cells of the lungs' airways and open up the airways in asthmatic lung tissues, researchers have identified a drug called TSG12. TSG12 is a specific transgelin-2 (TG2)-agonist that relaxes airway smooth muscle cells and reduces asthmatic pulmonary resistance. The authors claim that "TSG12 is both non-toxic and more effective in reducing pulmonary resistance than current bronchodilators and could be a promising therapeutic approach for treating asthma without losing effectiveness over time."
References
External links
Drug information
{{Respiratory physiology
Respiratory physiology
Respiratory therapy
Pulmonary function testing