Umeclidinium bromide

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Umeclidinium bromide
Umeclidinium bromide.svg
Umeclidinium bromide 3D.png
Clinical data
Trade names Incruse Ellipta
Other namesGSK573719A
License data
Routes of
administration
Inhalation (DPI)
ATC code
Legal status
Legal status
  • US: ℞-only
  • In general: ℞ (Prescription only)
Pharmacokinetic data
Protein binding ~89% [1]
Metabolism Hepatic (CYP2D6)
Elimination half-life 11 hours
Excretion Feces (58%) and urine (22%)
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
ChEBI
CompTox Dashboard (EPA)
ECHA InfoCard 100.166.375 OOjs UI icon edit-ltr-progressive.svg
Chemical and physical data
Formula C29H34BrNO2
Molar mass 508.500 g·mol−1
3D model (JSmol)

Umeclidinium bromide (trade name Incruse Ellipta) is a long-acting muscarinic antagonist approved for the maintenance treatment of chronic obstructive pulmonary disease (COPD). [1] It is also approved for this indication in combination with vilanterol (as umeclidinium bromide/vilanterol) [2] [3] and also as a triple-therapy combination as fluticasone furoate/umeclidinium bromide/vilanterol. [4]

Related Research Articles

Fluticasone/salmeterol

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

Salmeterol

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.

Beta<sub>2</sub>-adrenergic agonist

β2 (beta2) adrenergic receptor 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, such as Chronic obstructive pulmonary disease (COPD).

Long-acting beta-adrenoceptor agonist

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.

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 disease (COPD). It is delivered as an aerosol formulation through a dry powder inhaler.

Fluticasone furoate

Fluticasone furoate 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.

Aclidinium bromide

Aclidinium bromide (INN) is a long-acting, inhaled muscarinic antagonist (LAMA) approved in the United States on July 24, 2012 as a maintenance treatment for chronic obstructive pulmonary disease (COPD).

Tiotropium bromide

Tiotropium bromide, sold under the brand name Spiriva among others, is a long-acting bronchodilator used in the management of chronic obstructive pulmonary disease (COPD) and asthma. Specifically it is used to try to prevent periods of worsening rather than for those periods themselves. It is used by inhalation through the mouth. Onset typically begins within half an hour and lasts for 24 hours.

Chronic obstructive pulmonary disease Lung disease involving long-term poor airflow

Chronic obstructive pulmonary disease (COPD) is a type of obstructive lung disease characterized by long-term breathing problems and poor airflow. The main symptoms include shortness of breath and cough with sputum production. COPD is a progressive disease, meaning it typically worsens over time. Eventually, everyday activities such as walking or getting dressed become difficult. Chronic bronchitis and emphysema are older terms used for different types of COPD. The term "chronic bronchitis" is still used to define a productive cough that is present for at least three months each year for two years. Those with such a cough are at a greater risk of developing COPD. The term "emphysema" is also used for the abnormal presence of air or other gas within tissues.

Vilanterol

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).

Fluticasone furoate/vilanterol

Fluticasone furoate/vilanterol (FF/VI), sold under the trade names 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).

Umeclidinium bromide/vilanterol

Umeclidinium bromide/vilanterol, sold under the brand name Anoro Ellipta, among others, is a fixed-dose combination medication for the treatment of chronic obstructive pulmonary disease (COPD). It is applied as an inhalation.

Ellipta is part of GlaxoSmithKline's trade names of several inhalable asthma and chronic obstructive airway disease (COPD) combination medications that make use of the same type of inhaler:

Indacaterol/glycopyrronium bromide

Indacaterol/glycopyrronium bromide, sold under the brand name Ultibro Breezhaler among others, is a fixed-dose combination medication for inhalation consisting of the following two active ingredients:

Aclidinium bromide/formoterol, sold under the brand names Duaklir and Brimica, is a fixed-dose combination medication for inhalation, used in the management of chronic obstructive pulmonary disease (COPD). It consists of aclidinium bromide, a long-acting muscarinic antagonist, and formoterol, a long-acting β2 agonist.

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). It contains beclometasone dipropionate, formoterol fumarate dihydrate, and glycopyrronium bromide.

Fluticasone furoate/umeclidinium bromide/vilanterol (FF/UMEC/VI), 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 combination product contains medications that all 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).

Glycopyrronium bromide/formoterol, sold under the brand name Bevespi Aerosphere, is a combination medication for the maintenance treatment of chronic obstructive pulmonary disease (COPD). It is a combination of glycopyrronium bromide and formoterol. It is inhaled.

Budesonide/glycopyrronium bromide/formoterol, sold under the brand name Breztri Aerosphere is an inhalable fixed-dose combination medication for the treatment of chronic obstructive pulmonary disease (COPD). It contains budesonide, glycopyrronium bromide, and formoterol fumarate dihydrate. It is inhaled.

References

  1. 1 2 "Incruse Ellipta (umeclidinium inhalation powder) for Oral Inhalation Use. Full Prescribing Information" (PDF). GlaxoSmithKline, Research Triangle Park, NC 27709. Retrieved 22 February 2016.
  2. Feldman GJ, Edin A (December 2013). "The combination of umeclidinium bromide and vilanterol in the management of chronic obstructive pulmonary disease: current evidence and future prospects". Therapeutic Advances in Respiratory Disease. 7 (6): 311–9. doi:10.1177/1753465813499789. PMID   24004659. S2CID   5744282.
  3. "FDA Approves Umeclidinium and Vilanterol Combo for COPD". Medscape. December 18, 2013.
  4. "TRELEGY ELLIPTA Package Insert" (PDF). GlaxoSmithKline. September 2017. Retrieved 11 July 2020.