Salmeterol
Clinical data | |
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Trade names | Serevent, Aeromax, Qitai, others |
AHFS/Drugs.com | Monograph |
License data |
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Pregnancy category |
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Routes of administration | Respiratory inhalation (Metered-dose inhaler (MDI), Dry-powder inhaler (DPI)) |
ATC code | |
Legal status | |
Legal status | |
Pharmacokinetic data | |
Protein binding | 96% |
Metabolism | Liver (CYP3A4) |
Elimination half-life | 5.5 hours |
Identifiers | |
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JSmol) | |
Chirality | Racemic mixture |
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Salmeterol is a
It was patented in 1983 and came into medical use in 1990.[4] It is marketed as Serevent in the US.[5] It is available as a dry-powder inhaler (DPI) that releases a powdered form of the drug. It was previously available as a metered-dose inhaler (MDI) but was discontinued in the US in 2002.[2][6] It is available as an MDI in other countries as of 2020.[7]
Mechanism of action
Inhaled salmeterol belongs to a group of drugs called
The primary noticeable difference of salmeterol from
Medical uses
- Salmeterol is used in moderate-to-severe persistent asthma following previous treatment with a short-acting β2 adrenoreceptor agonist (SABA) such as salbutamol (albuterol).
- LABAs should not be used as a monotherapy, instead, they should be used concurrently with an inhaled corticosteroid, such as beclometasone dipropionate or fluticasone propionate in the treatment of asthmato minimize serious reactions such as asthma-related deaths. Combination of inhaled corticosteroids and salmeterol (LABA) has synergistic action and reduces the frequency of asthma attacks and also makes it less severe.
- In chronic obstructive pulmonary disease (COPD), LABAs may be used as monotherapy or in combination with corticosteroids. The Torch study demonstrated benefits in terms of quality of life and lung function of salmeterol alone or in combination with inhaled corticosteroids in patients with COPD[11]
- In exercise-induced bronchospasm monotherapy may be indicated in patients without persistent asthma. LABAs should not be used to treat acute symptoms.[2][9][12]
Pregnancy and lactation
Salmeterol use during pregnancy must be decided based on the risks versus benefits to the mother. There are no well-controlled studies with salmeterol in pregnant women. Some animal studies showed developmental malformation when the mother was given several clinical doses orally. In rats, salmeterol xinafoate is excreted in the milk. However, since there is no data to show excretion of salmeterol in a mother's breast milk, a decision on whether to continue or discontinue therapy should be decided based on the important benefits it provides to the mother. Pregnant and lactating women should consult their doctors before using salmeterol.[1]
Side effects
Due to its vasodilation properties, the common side effects of salmeterol are
Other side effects
- muscle tremors,
- hypokalemia due to direct effect on beta-2 receptors on skeletal muscle.
In most cases, salmeterol side effects are minor and either do not require treatment or can easily be treated. Certain side effects, however, should be reported to a healthcare provider immediately.
Some of these more serious side effects include
- very fast heart rate,
- high blood pressure, and
- worsening breathing problems.[13]
Structure-activity relationship
Salmeterol has an
History
Salmeterol, first marketed and manufactured by
In November 2005, the US Food and Drug Administration (FDA) released a health advisory, alerting the public to findings that show the use of long-acting β2 agonists could lead to a worsening of symptoms, and in some cases death.[15]
While the use of inhaled LABAs are still recommended in asthma guidelines for the resulting improved symptom control,[16] further concerns have been raised. A large meta-analysis of pooled results from 19 trials with 33,826 participants, suggests that salmeterol may increase the small risks of asthma-related deaths, and this additional risk is not reduced with the additional use of inhaled steroids (e.g., as with the combination product fluticasone/salmeterol).[17] This seems to occur because although LABAs relieve asthma symptoms, they also promote bronchial inflammation and sensitivity without warning.[18]
Society and culture
Names
Combinations of inhaled steroids and these long-acting bronchodilators are becoming[when?] more widespread; the most common combination currently[when?] in use is fluticasone/salmeterol (brand names Seretide (UK) and Advair (US)). Another combination is budesonide/formoterol (brand name Symbicort).[19]
References
- ^ a b "Serevent Diskus- salmeterol xinafoate powder, metered". DailyMed. 13 January 2020. Retrieved 6 September 2020.
- ^ a b c d "global initiative for chronic obstructive disease" (PDF). goldcopd.org. Archived from the original (PDF) on 24 September 2015. Retrieved 30 October 2014.
- ^ a b "National Asthma Education and Prevention Program". Retrieved 30 October 2014.
- ISBN 9783527607495.
- ^ "Salmeterol inhalation index". Retrieved 30 October 2014.
- ^ a b "Benefit Risk Assessment of Salmeterol for the Treatment of Asthma in Adults and Children" (PDF). fda.gov. Archived from the original (PDF) on 26 January 2018.
- ^ "Serevent Dosieraeros 25 mcg FCKW-frei". compendium.ch (in German). Archived from the original on 2021-07-24. Retrieved 2020-03-25.
- )
- ^ a b "Global initiative for asthma" (PDF). ginasthma.org. Archived from the original (PDF) on 22 August 2014. Retrieved 30 October 2014.
- ^ "Recommended Medication for Asthma" (PDF). www.partnershiphp.org. Archived from the original (PDF) on 2014-11-03.
- PMID 17314337.
- ^ "Use of long-acting beta agonist in chronic obstructive pulmonary disease". mhra.gov.uk. Archived from the original on 3 November 2014. Retrieved 30 October 2014.
- ^ "Medtv". HealthSavy. Retrieved 8 March 2012.
- ^ Mehta A. "Medicinal Chemistry of Adrenergics and Cholinergics". PharmaXChange. Archived from the original on 2010-11-04.
- ^ "Advair Diskus, Advair HFA, Brovana, Foradil, Perforomist, Serevent Diskus, and Symbicort Information (Long Acting Beta Agonists)". Fierce Biotech. 6 March 2008.
- ^ British Thoracic Society & Scottish Intercollegiate Guidelines Network (SIGN). British Guideline on the Management of Asthma. Guideline No. 63. Edinburgh:SIGN; 2004. (HTML Archived 2006-06-18 at the Wayback Machine, Full PDF Archived 2006-07-24 at the Wayback Machine, Summary PDF Archived 2006-07-24 at the Wayback Machine)
- PMID 16754916.
- ^ Ramanujan K (June 9, 2006). "Common asthma inhalers cause up to 80 percent of asthma-related deaths, Cornell and Stanford researchers assert". ChronicalOnline - Cornell University.
- ^ "Australian Medicines Handbook". amhonline.amh.net.au. Retrieved 2020-05-07.
External links
- "Salmeterol". Drug Information Portal. U.S. National Library of Medicine.