Bronchodilator

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Bronchodilator
Specialty Pulmonology

A bronchodilator or broncholytic [1] (although the latter occasionally includes secretory inhibition as well) is a substance that dilates the bronchi and bronchioles, decreasing resistance in the respiratory airway and increasing airflow to the lungs. Bronchodilators may be originating naturally within the body, or they may be medications administered for the treatment of breathing difficulties, usually in the form of inhalers. They are most useful in obstructive lung diseases, of which asthma and chronic obstructive pulmonary disease are the most common conditions. Although this remains somewhat controversial, they might be useful in bronchiolitis and bronchiectasis. They are often prescribed but of unproven significance in restrictive lung diseases. [2]

Contents

Bronchodilators are either short-acting or long-acting. Short-acting medications provide quick or "rescue" relief from acute bronchoconstriction. Long-acting bronchodilators help to control and prevent symptoms. The three types of prescription bronchodilating drugs are beta-2 adrenergic agonists (short- and long-acting), anticholinergics (short- and long-acting), and theophylline (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 β2-adrenergic agonists and can relieve bronchospasms without unwanted cardiac side effects of nonspecific β-agonists (for example, ephedrine or epinephrine). Patients who regularly or frequently need to take a short-acting β2-adrenergic agonist should consult their doctor, as such usage indicates uncontrolled asthma, and their routine medications may need adjustment.[ citation needed ]

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.[ citation needed ]

Salmeterol and formoterol are examples of these.

Anticholinergics

Some examples of anticholinergics are tiotropium (Spiriva) and ipratropium bromide.[ citation needed ]

Tiotropium is a long-acting, 24-hour, anticholinergic bronchodilator used in the management of chronic obstructive pulmonary disease (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. [3] 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 β2-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 β2-adrenergic agonists has been shown to reduce hospital admissions in children and adults with acute asthma exacerbations. [4] [5]

Other

Available in oral and injectable form, theophylline is a long-acting bronchodilator that prevents asthma episodes. It belongs to the chemical class methylxanthines (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, 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, [6] methamphetamine, and cocaine, [7] have bronchodilating effects and were used often for asthma due to the lack of effective β2-adrenergic agonists for use as bronchodilator, but are now rarely, if ever, used medically for their bronchodilatory effects.

Gaseous carbon dioxide also relaxes airway musculature: hypocapnia caused by deliberate hyperventilation increases respiratory resistance while hypercapnia induced by carbon dioxide inhalation reduces it; [8] however, this bronchodilating effect of carbon dioxide inhalation only lasts 4 to 5 minutes. [9] Nonetheless, this observation has inspired the development of S-1226, carbon dioxide-enriched air formulated with nebulized perflubron. [10]

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:

Long-acting bronchodilators include

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." [11] [12]

Related Research Articles

<span class="mw-page-title-main">Asthma</span> Long-term inflammatory disease of the airways of the lungs

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, coughing, chest tightness, and shortness of breath. These may occur a few times a day or a few times per week. Depending on the person, asthma symptoms may become worse at night or with exercise.

<span class="mw-page-title-main">Salbutamol</span> Medication

Salbutamol, also known as albuterol and sold under the brand name Ventolin among others, is a medication that opens up the medium and large airways in the lungs. It is a short-acting β2 adrenergic receptor agonist that causes relaxation of airway smooth muscle. It is used to treat asthma, including asthma attacks and exercise-induced bronchoconstriction, as well as chronic obstructive pulmonary disease (COPD). It may also be used to treat high blood potassium levels. Salbutamol is usually used with an inhaler or nebulizer, but it is also available in a pill, liquid, and intravenous solution. Onset of action of the inhaled version is typically within 15 minutes and lasts for two to six hours.

<span class="mw-page-title-main">Bronchospasm</span> Lower respiratory tract disease that affects the airways leading into the lungs

Bronchospasm or a bronchial spasm is a sudden constriction of the muscles in the walls of the bronchioles. It is caused by the release (degranulation) of substances from mast cells or basophils under the influence of anaphylatoxins. It causes difficulty in breathing which ranges from mild to severe.

<span class="mw-page-title-main">Ipratropium bromide</span> Type of anticholinergic

Ipratropium bromide, sold under the trade name Atrovent among others, is a type of anticholinergic medication which opens up the medium and large airways in the lungs. It is used to treat the symptoms of chronic obstructive pulmonary disease and asthma. It is used by inhaler or nebulizer. Onset of action is typically within 15 to 30 minutes and lasts for three to five hours.

<span class="mw-page-title-main">Salmeterol</span> Chemical compound

Salmeterol 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 bronchospasm include shortness of breath, wheezing, coughing and chest tightness. It is also used to prevent breathing difficulties during exercise.

<span class="mw-page-title-main">Formoterol</span> Chemical compound

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 compared to short-acting β2 agonists such as salbutamol (albuterol), which are effective for 4 h to 6 h. Formoterol has a relatively rapid onset of action compared to other LABAs, and is effective within 2-3 minutes. The 2022 Global Initiative for Asthma report recommends a combination formoterol/inhaled corticosteroid inhaler as both a preventer and reliever treatment for asthma in adults. In children, a short-actingβ2 agonist is still recommended.

Beta<sub>2</sub>-adrenergic agonist Compounds that bind to and activate adrenergic beta-2 receptors

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' effects on smooth muscle cause dilation of bronchial passages, vasodilation in muscle and liver, relaxation of uterine muscle, and release of insulin. They are primarily used to treat asthma and other pulmonary disorders. Bronchodilators are considered an important treatment regime for Chronic obstructive pulmonary disease (COPD) and are usually used in combination with short acting medications and long acting medications in a combined inhaler.

<span class="mw-page-title-main">Bronchoconstriction</span> Constriction of the terminal airways in the lungs

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.

<span class="mw-page-title-main">Long-acting beta-adrenoceptor agonist</span> Drug prescribed for asthma patients

Long-acting β adrenoceptor agonists are usually prescribed for moderate-to-severe persistent asthma patients or patients with chronic obstructive pulmonary disease (COPD). They are designed to reduce the need for shorter-acting β2 agonists such as salbutamol (albuterol), as they have a duration of action of approximately 12 hours in comparison with the 4-to-6-hour duration of salbutamol, making them candidates for sparing high doses of corticosteroids or treating nocturnal asthma and providing symptomatic improvement in patients with COPD. With the exception of formoterol, long-acting β2 agonists are not recommended for the treatment of acute asthma exacerbations because of their slower onset of action compared to salbutamol. Their long duration of action is due to the addition of a long, lipophilic side-chain that binds to an exosite on adrenergic receptors. This allows the active portion of the molecule to continuously bind and unbind at β2 receptors in the smooth muscle in the lungs.

Exercise-induced bronchoconstriction (EIB) occurs when the airways narrow as a result of exercise. This condition has been referred to as exercise-induced asthma (EIA), however this term is no longer preferred. While exercise does not cause asthma, it is frequently an asthma trigger.

<span class="mw-page-title-main">Levosalbutamol</span> Chemical compound

Levosalbutamol, also known as levalbuterol, is a short-acting β2 adrenergic receptor agonist used in the treatment of asthma and chronic obstructive pulmonary disease (COPD). Evidence is inconclusive regarding the efficacy of levosalbutamol versus salbutamol or salbutamol-levosalbutamol combinations, though levosalbutamol is believed to have a better safety profile due to its more selective binding to β2 receptors versus β1.

<span class="mw-page-title-main">Bitolterol</span> Chemical compound

Bitolterol mesylate (Tornalate) is a short-acting β2 adrenergic receptor agonist used for the relief of bronchospasm in conditions such as asthma and COPD. In these disorders there is a narrowing of the airways that carry air to the lungs. Muscle spasm and inflammation within the bronchi worsen this narrowing. Bitolterol relaxes the smooth muscles present continuously around the bronchi and bronchioles facilitating the flow of air through them.

<span class="mw-page-title-main">Pirbuterol</span> Chemical compound

Pirbuterol is a short-acting β2 adrenoreceptor agonist with bronchodilating action used in the treatment of asthma, available as a breath-activated metered-dose inhaler.

<span class="mw-page-title-main">Acute exacerbation of chronic obstructive pulmonary disease</span> Medical condition

An acute exacerbation of chronic obstructive pulmonary disease, or acute exacerbations of chronic bronchitis (AECB), is a sudden worsening of chronic obstructive pulmonary disease (COPD) symptoms including shortness of breath, quantity and color of phlegm that typically lasts for several days.

<span class="mw-page-title-main">Chronic obstructive pulmonary disease</span> Lung disease involving long-term poor airflow

Chronic obstructive pulmonary disease (COPD) is a type of progressive lung disease characterized by long-term respiratory symptoms and airflow limitation. GOLD 2024 defined COPD as a heterogeneous lung condition characterized by chronic respiratory symptoms due to abnormalities of the airways and/or alveoli (emphysema) that cause persistent, often progressive, airflow obstruction.

<span class="mw-page-title-main">Olodaterol</span> Chemical compound

Olodaterol is an ultra-long-acting β adrenoreceptor agonist (ultra-LABA) used as an inhalation for treating people with chronic obstructive pulmonary disease (COPD). It is manufactured by Boehringer Ingelheim.

β2-adrenoceptor agonists are a group of drugs that act selectively on β2-receptors in the lungs causing bronchodilation. β2-agonists are used to treat asthma and COPD, diseases that cause obstruction in the airways. Prior to their discovery, the non-selective beta-agonist isoprenaline was used. The aim of the drug development through the years has been to minimise side effects, achieve selectivity and longer duration of action. The mechanism of action is well understood and has facilitated the development. The structure of the binding site and the nature of the binding is also well known, as is the structure activity relationship.

Fluticasone furoate/umeclidinium bromide/vilanterol, sold under the brand name Trelegy Ellipta among others, is a fixed-dose combination inhaled medication that is used for the maintenance treatment of chronic obstructive pulmonary disease (COPD). The medications work in different ways: fluticasone furoate is an inhaled corticosteroid (ICS), umeclidinium is a long-acting muscarinic antagonist (LAMA), and vilanterol is a long-acting beta-agonist (LABA).

Tedral is a medicine formerly used to treat respiratory diseases such as asthma, chronic obstructive lung disease (COPD), chronic bronchitis, and emphysema. It is a combination drug containing three active ingredients - theophylline, ephedrine, phenobarbital. This medication relaxes the smooth muscle of the airways, making breathing easier. The common side effects of Tedral include gastrointestinal disturbances, dizziness, headache and lightheadedness. However, at high dose, it may lead to cardiac arrhythmias, hypertension, seizures or other serious cardiovascular and/or central nervous system adverse effects. Tedral is contraindicated in individuals with hypersensitivity to theophylline, ephedrine and/or phenobarbital. It should be also used in caution in patients with cardiovascular complications, such as ischemic heart disease and heart failure and/or other disease conditions. It can cause a lot of drug–drug interactions. Therefore, before prescribing patient with Tedral, drug interactions profile should be carefully checked if the patient had other concurrent medication(s). Being used as a treatment option for respiratory diseases for decades, Tedral was withdrawn from the US market in 2006 due to safety concerns.

Airway tone, short for airway smooth muscle tone, is the degree of sustained contractile activation of airway smooth muscle. The airways have a tone baseline, and consequently a baseline level of contraction of their smooth musculature. Airway tone is a key determinant of lung function and the presence of respiratory symptoms in obstructive lung diseases such as asthma, where baseline airway tone is elevated. The upper extreme of the spectrum of airway tone represents bronchoconstriction, wherein the airway smooth muscles are significantly contracted, while the lower extreme represents bronchodilatation, wherein the muscles are relatively relaxed.

References

  1. ↑ Venes, Donald (2017-01-25). Taber's Cyclopedic Medical Dictionary. F.A. Davis. ISBN   9780803659407.
  2. ↑ Sathe NA, Krishnaswami S, Andrews J, Ficzere C, McPheeters ML (July 2015). "Pharmacologic Agents That Promote Airway Clearance in Hospitalized Subjects: A Systematic Review" (PDF). Respiratory Care. 60 (7): 1061–70. doi: 10.4187/respcare.04086 . PMID   25944943. S2CID   7017557.
  3. ↑ Price D, Fromer L, Kaplan A, van der Molen T, Román-Rodríguez M (July 2014). "Is there a rationale and role for long-acting anticholinergic bronchodilators in asthma?". npj Primary Care Respiratory Medicine. 24 (1): 14023. doi:10.1038/npjpcrm.2014.23. PMC   4373380 . PMID   25030457.
  4. ↑ Rodrigo GJ, Castro-Rodriguez JA (September 2005). "Anticholinergics in the treatment of children and adults with acute asthma: a systematic review with meta-analysis". Thorax. 60 (9): 740–6. doi:10.1136/thx.2005.040444. PMC   1747524 . PMID   16055613.
  5. ↑ Griffiths B, Ducharme FM (December 2013). "Combined inhaled anticholinergics and short-acting beta2-agonists for initial treatment of acute asthma in children". Paediatric Respiratory Reviews. 14 (4): 234–5. doi:10.1016/j.prrv.2013.08.002. PMID   24070913.
  6. ↑ Amphetamine is listed as having medical uses as bronchodilator. Medic8
  7. ↑ Streatfeild D (17 June 2003). Cocaine: An Unauthorized Biography. Macmillan. p. 110. ISBN   978-0-312-42226-4 . Retrieved 14 February 2011.
  8. ↑ van den Elshout, F. J.; van Herwaarden, C. L.; Folgering, H. T. (January 1991). "Effects of hypercapnia and hypocapnia on respiratory resistance in normal and asthmatic subjects". Thorax. 46 (1): 28–32. doi:10.1136/thx.46.1.28. ISSN   0040-6376. PMC   1020910 . PMID   1908137.
  9. ↑ Fisher, H. K.; Hansen, T. A. (November 1976). "Site of action of inhaled 6 per cent carbon dioxide in the lungs of asthmatic subjects before and after exercise". The American Review of Respiratory Disease. 114 (5): 861–870. doi:10.1164/arrd.1976.114.5.861 (inactive 31 January 2024). ISSN   0003-0805. PMID   984580.{{cite journal}}: CS1 maint: DOI inactive as of January 2024 (link)
  10. ↑ Green, Francis H. Y.; Leigh, Richard; Fadayomi, Morenike; Lalli, Gurkeet; Chiu, Andrea; Shrestha, Grishma; ElShahat, Sharif G.; Nelson, David Evan; El Mays, Tamer Y.; Pieron, Cora A.; Dennis, John H. (2016-07-28). "A phase I, placebo-controlled, randomized, double-blind, single ascending dose-ranging study to evaluate the safety and tolerability of a novel biophysical bronchodilator (S-1226) administered by nebulization in healthy volunteers". Trials. 17: 361. doi: 10.1186/s13063-016-1489-8 . ISSN   1745-6215. PMC   4964056 . PMID   27464582.
  11. ↑ New drug therapy could lead to more effective treatment for millions with asthma
  12. ↑ Yin, Lei-Miao; Xu, Yu-Dong; Peng, Ling-Ling; Duan, Ting-Ting; Liu, Jia-Yuan; Xu, Zhijian; Wang, Wen-Qian; Guan, Nan; Han, Xiao-Jie; Li, Hai-Yan; Pang, Yu; Wang, Yu; Chen, Zhaoqiang; Zhu, Weiliang; Deng, Linhong; Wu, Ying-Li; Ge, Guang-Bo; Huang, Shuang; Ulloa, Luis; Yang, Yong-Qing (2018). "Transgelin-2 as a therapeutic target for asthmatic pulmonary resistance". Science Translational Medicine. 10 (427). doi:10.1126/scitranslmed.aam8604. PMC   6310021 . PMID   29437149.
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