Fluticasone/salmeterol

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Fluticasone/salmeterol
Fluticasone propionate and salmeterol.svg
Fluticasone propionate (top) and salmeterol (bottom)
Combination of
Fluticasone propionate Glucocorticoid
Salmeterol Long-acting β2 agonist (LABA)
Clinical data
Trade names Advair, Seretide, Cyplos, others
AHFS/Drugs.com FDA Professional Drug Information
MedlinePlus a699063
License data
Pregnancy
category
  • AU:B3
Routes of
administration 		Inhalation
ATC code
Legal status
Legal status
  • AU: S4 (Prescription only) [1]
  • CA: ℞-only
  • UK: POM (Prescription only)
  • US: ℞-only
  • EU:Rx-only
  • In general: ℞ (Prescription only)
Identifiers
CAS Number
PubChem CID
ChemSpider
KEGG
   (verify)

Fluticasone/salmeterol, sold under the brand name Advair among others, is a fixed-dose combination medication containing fluticasone propionate and salmeterol. [2] It is used in the management of asthma and chronic obstructive pulmonary disease (COPD). [2] It is used by inhaling the medication into the lungs. [2]

Contents

Common side effects include thrush, headache, and cough. [3] Serious side effects may include worsening asthma, anaphylaxis, seizures, and heart problems. [3] Safety in pregnancy and breastfeeding is unclear. [4] Fluticasone, a corticosteroid, works by decreasing inflammation while salmeterol, a long-acting beta-adrenoceptor agonist (LABA), works by activating beta-2 adrenergic receptors. [3]

The combination was approved for medical use in the United States in 2000. [3] A generic version was approved in the United States in 2019. [5] In 2021, it was the 64th most commonly prescribed medication in the United States, with more than 10 million prescriptions. [6] [7]

Medical uses

Fluticasone, a corticosteroid, is the anti-inflammatory component of the combination which decreases inflammation in the lungs. This leads to improvement in breathing. Salmeterol, an LABA, treats constriction of the airways. The combination of both is meant to be used as maintenance therapy and not as a rescue therapy for sudden symptoms.

Side effects

The common side effects of this combination are those of its individual drugs. For instance, the use of inhaled corticosteroids is associated with oral candidiasis, commonly known as yeast infection or thrush. Rinsing the mouth with water after inhaling the medication decreases the risk of developing this condition.

While the use of inhaled steroids and LABA are recommended for the resulting improvement in control of symptoms of asthma, [8] concerns have been raised that salmeterol may increase the risk of death due to asthma, and this additional risk is not reduced by the addition of inhaled steroids. [9] Other side effects from this drug combination may include increased blood pressure, change in heart rate, an irregular heartbeat, increased risk of osteoporosis, cataracts, and glaucoma. [10] Studies have demonstrated the safety of inhaled fluticasone propionate in children. A systematic review published in 2013 found no significant adverse effect on the function of the hypothalamic–pituitary–adrenal axis, growth, and bone mineral density in asthmatic children when inhaled fluticasone is used for up to three months. [11]

Mechanism of action

Fluticasone/salmeterol contains fluticasone propionate, a synthetic corticosteroid, and salmeterol, a selective long-acting beta-adrenergic receptor agonist. Fluticasone works as a potent anti-inflammatory agent, inhibiting multiple cell types such as mast cells, eosinophils, basophils, lymphocytes, macrophages, and neutrophils all of which contribute to inflammation, a large component in the pathogenesis of asthma. Salmeterol works by stimulating intracellular adenyl cyclase, which acts as a catalyst in the production of cyclic AMP. Increased cyclic AMP levels lead to a relaxation of bronchial smooth muscles. Additionally, cyclic AMP inhibits the release of mediators of immediate hypersensitivity. [12]

Society and culture

On 28 January 2021, the Committee for Medicinal Products for Human Use (CHMP) of the European Medicines Agency (EMA) adopted a positive opinion, recommending the granting of a marketing authorization for the medicinal product Seffalair Spiromax, intended for the treatment of asthma. [13] The applicant for this medicinal product is Teva B.V. [13] The CHMP also recommended the granting of a marketing authorization for the duplicate product BroPair Spiromax. [14] Seffalair Spiromax and BroPair Spiromax were both approved for medical use in the European Union in March 2021. [15] [16] [17] [18]

Generic equivalents

In January 2019, the FDA granted Mylan N.V. the first generic approval for Advair Diskus. [19]

Civil settlements

In 2012, Advair was part of a larger civil settlement agreement between GlaxoSmithKline (GSK) and the United States, in which GSK agreed to pay $1.043 billion; the United States said that GSK promoted off-label uses of Advair and paid kickbacks to healthcare professionals to sell this drug, among others. [20]

Related Research Articles

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

Fluticasone is a manufactured glucocorticoid used to treat nasal symptoms. Both the esters, fluticasone propionate and fluticasone furoate, are also used as topical anti-inflammatories and inhaled corticosteroids, and are used much more commonly in comparison.

<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">Budesonide/formoterol</span> Medication for asthma & chronic obstructive pulmonary disease

Budesonide/formoterol, sold under the brand name Symbicort among others, is a fixed-dose combination medication used in the management of asthma or chronic obstructive pulmonary disease (COPD). It contains budesonide, a steroid and formoterol, a long-acting β2-agonist (LABA). The product monograph does not support its use for sudden worsening or treatment of active bronchospasm. However, a 2020 review of the literature does support such use. It is used by breathing in the medication.

<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-acting β2 adrenergic 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">Fluticasone propionate</span> Medication

Fluticasone propionate, sold under the brand names Flovent and Flonase among others, is a steroid medication. When inhaled it is used for the long term management of asthma and COPD. In the nose it is used for hay fever and nasal polyps. It can also be used for mouth ulcers. It works by decreasing inflammation.

<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 (LABAs) are beta-adrenergic agonists usually prescribed for moderate-to-severe persistent asthma and 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.

<span class="mw-page-title-main">Mometasone</span> Steroid medication

Mometasone, also known as mometasone y 3 s, is a steroid medication used to treat certain skin conditions, hay fever, and asthma. Specifically it is used to prevent rather than treat asthma attacks. It can be applied to the skin, inhaled, or used in the nose. Mometasone furoate, not mometasone, is used in medical products.

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

Fluticasone furoate, sold under the brand name Flonase Sensimist among others, is a corticosteroid for the treatment of non-allergic and allergic rhinitis administered by a nasal spray. It is also available as an inhaled corticosteroid to help prevent and control symptoms of asthma. It is derived from cortisol. Unlike fluticasone propionate, which is only approved for children four years and older, fluticasone furoate is approved in children as young as two years of age when used for allergies.

<span class="mw-page-title-main">Budesonide</span> Type of corticosteroid medication; group of stereoisomers

Budesonide, sold under the brand name Pulmicort among others, is a medication of the corticosteroid type. It is available as an inhaler, nebulization solution, pill, nasal spray, and rectal forms. The inhaled form is used in the long-term management of asthma and chronic obstructive pulmonary disease (COPD). The nasal spray is used for allergic rhinitis and nasal polyps. The pills in a delayed release form and rectal forms may be used for inflammatory bowel disease including Crohn's disease, ulcerative colitis, and microscopic colitis.

<span class="mw-page-title-main">Mometasone/formoterol</span> Combination drug

Mometasone/formoterol, sold under the brand name Dulera among others, is a fixed-dose combination medication used in the long-term treatment of asthma. It contains mometasone a steroid and formoterol a long-acting beta agonist. It is only recommended in those for whom an inhaled steroid is not sufficient. It is used by inhalation.

<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.

<span class="mw-page-title-main">Vilanterol</span> Asthma drug – β2 adrenoreceptor agonist

Vilanterol is an ultra-long-acting β2 adrenoreceptor agonist (ultra-LABA), which was approved in May 2013 in combination with fluticasone furoate for sale as Breo Ellipta by GlaxoSmithKline for the treatment of chronic obstructive pulmonary disease (COPD).. The combination is also approved for the treatment of asthma in Canada, Europe, Japan and New Zealand.

<span class="mw-page-title-main">Fluticasone furoate/vilanterol</span> Pharmaceutical drug formulation

Fluticasone furoate/vilanterol, sold under the brand name Breo Ellipta among others, is a combination medication for the treatment of chronic obstructive pulmonary disease (COPD) and asthma. It contains fluticasone furoate, an inhaled corticosteroid, and vilanterol, an ultra-long-acting β2 agonist (ultra-LABA).

Beclometasone/formoterol/glycopyrronium, sold under the brand name Trimbow among others, is an inhalable fixed-dose combination medication for the treatment of chronic obstructive pulmonary disease (COPD) and asthma. It contains beclometasone dipropionate, formoterol fumarate dihydrate, and glycopyrronium bromide.

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).

Indacaterol/mometasone, sold under the brand name Atectura Breezhaler among others, is a fixed-dose combination medication for the treatment of asthma in adults and adolescents twelve years of age and older not adequately controlled with inhaled corticosteroids and inhaled short acting beta2 agonists.

Indacaterol/glycopyrronium bromide/mometasone, sold under the brand name Enerzair Breezhaler among others, is an inhalable fixed-dose combination medication for the treatment of asthma. It contains indacaterol as acetate, glycopyrronium bromide, and mometasone furoate.

Salbutamol/budesonide, sold under the brand name Airsupra, is a fixed-dose combination medication for the treatment of bronchoconstriction and asthma. It is a combination of salbutamol sulfate, a short-acting beta2-adrenergic agonist, and budesonide, an inhaled corticosteroid. It is inhaled using a pressurized metered-dose inhaler.

References

  1. ↑ "Seroflo Multihaler (Cipla Australia Pty Ltd)". Department of Health and Ages Care. Retrieved 1 April 2023.
  2. 1 2 3 British national formulary : BNF 76 (76 ed.). Pharmaceutical Press. 2018. pp. 263–264. ISBN   9780857113382.
  3. 1 2 3 4 "Fluticasone and Salmeterol inhalation - FDA prescribing information, side effects and uses". Drugs.com. Retrieved 4 March 2019.
  4. ↑ "Fluticasone / salmeterol Pregnancy and Breastfeeding Warnings". Drugs.com. Retrieved 3 March 2019.
  5. ↑ Office of the Commissioner. "Press Announcements - FDA approves first generic Advair Diskus". www.fda.gov. Retrieved 1 February 2019.
  6. ↑ "The Top 300 of 2021". ClinCalc. Archived from the original on 15 January 2024. Retrieved 14 January 2024.
  7. ↑ "Fluticasone; Salmeterol - Drug Usage Statistics". ClinCalc. Retrieved 14 January 2024.
  8. ↑ "Guideline 101: British Guideline on the Management of Asthma". British Thoracic Society & Scottish Intercollegiate Guidelines Network (SIGN). Archived from the original on 18 April 2015.
  9. ↑ Salpeter SR, Buckley NS, Ormiston TM, Salpeter EE (June 2006). "Meta-analysis: effect of long-acting beta-agonists on severe asthma exacerbations and asthma-related deaths". Ann. Intern. Med. 144 (12): 904–12. doi: 10.7326/0003-4819-144-12-200606200-00126 . PMID   16754916.
  10. ↑ "US fluticasone propionate/Salmeterol label" (PDF). FDA. April 2016.
  11. ↑ Muley P, Shah M, Muley A (July 2013). "Safety of inhaled fluticasone propionate therapy for pediatric asthma - a systematic review". Current Drug Safety. 8 (3): 186–194. doi:10.2174/15748863113089990038. PMID   23859431.
  12. ↑ "Advair Diskus 100/50" (PDF). Food and Drug Administration. Retrieved 30 October 2019.
  13. 1 2 "Seffalair Spiromax: Pending EC decision". European Medicines Agency (EMA). 1 February 2021. Archived from the original on 10 February 2021. Retrieved 1 February 2021.
  14. ↑ "BroPair Spiromax: Pending EC decision". European Medicines Agency (EMA). 1 February 2021. Archived from the original on 13 April 2021. Retrieved 1 February 2021.
  15. ↑ "Seffalair Spiromax EPAR". European Medicines Agency (EMA). 25 January 2021. Retrieved 23 August 2021.
  16. ↑ "BroPair Spiromax EPAR". European Medicines Agency (EMA). 25 January 2021. Retrieved 23 August 2021.
  17. ↑ "Seffalair Spiromax Product information". Union Register of medicinal products. Retrieved 3 March 2023.
  18. ↑ "BroPair Spiromax Product information". Union Register of medicinal products. Retrieved 3 March 2023.
  19. ↑ "FDA approves first generic Advair Diskus". U.S. Food and Drug Administration (FDA). 24 March 2020.
  20. ↑ "GlaxoSmithKline to Plead Guilty and Pay $3 Billion to Resolve Fraud Allegations and Failure to Report Safety Data". Department of Justice: Office of Public Affairs. 2 July 2012.
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