Description

Simple

A medication used to treat lung conditions that lead to obstructed airways and breathing difficulties.

Clinical

A long-acting beta2-adrenergic agonist used in combination with other bronchodilators for the management of chronic obstructive pulmonary disease (COPD), including chronic bronchitis and/or emphysema.

Overview

Vilanterol is a selective long-acting beta2-adrenergic agonist (LABA) with inherent 24-hour activity for once daily treatment of COPD and asthma. Its pharmacological effect is attributable to stimulation of intracellular adenylyl cyclase which catalyzes the conversion of adenosine triphosphate (ATP) to cyclic-3',5'-adenosine monophosphate (cAMP). Increases in cyclic AMP are associated with relaxation of bronchial smooth muscle and inhibition of release of hypersensitivity mediators from mast cells in the lungs.

Vilanterol is approved for use in several combination products such as with fluticasone furoate under the tradename Breo Ellipta and in combination with umeclidinium bromide as Anoro Ellipta. Approved by the FDA in 2013, use of Breo Ellipta is indicated for the long-term, once-daily maintenance treatment of airflow obstruction in patients with COPD, including chronic bronchitis and emphysema. It is also indicated for once-daily maintenance treatment of asthma in patients aged 18 or older with reversible obstructive airways disease.

Pharmacology

Indication

Vilanterol is approved for use in several combination products such as with fluticasone furoate under the tradename Breo Ellipta and in combination with umeclidinium bromide as Anoro Ellipta. Approved by the FDA in 2013, use of Breo Ellipta is indicated for the long-term, once-daily maintenance trea... Read more

Pharmacodynamic

Information currently not available.

Mechanism of action

Vilanterol is a selective long-acting beta2-adrenergic agonist. Its pharmacological effect is attributable to stimulation of intracellular adenylyl cyclase which catalyzes the conversion of adenosine triphosphate (ATP) to cyclic-3',5'-adenosine monophosphate (cAMP). Increases in cyclic AMP are assoc... Read more

Absorption

Peak plasma concentrations are achieved within 10 minutes of inhalation. Absolute bioavailability was found to be 27.3% when administered by inhalation, whereas oral bioavailability was found to be less than 2% due to extensive first-pass metabolism. Systemic exposure is 24% higher in patients with... Read more

Protein binding

Binding to plasma protein was 93.9%.

Volume of distribution

Following IV administration to healthy subjects, the mean volume of distribution at steady state was 661 L.

Clearance

Information currently not available.

Half life

21.3 hr

Route of elimination

Following oral administration, vilanterol is eliminated mainly by metabolism by CYP3A4 followed by excretion of metabolites in urine (70%) and feces (30%).

Toxicity

Information currently not available.

Adverse Effects

Contraindications

  • Regions: US
  • Patient Conditions:
      • Name: Hypersensitivity to milk proteins
      • Drugbank Id: DBCOND0108555

Food Interactions

    Information currently not available.

Interactions

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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
1-benzylimidazole
The risk or severity of hypertension can be increased when 1-benzylimidazole is combined with Vilanterol.
2-Methoxyethanol
The risk or severity of adverse effects can be increased when 2-Methoxyethanol is combined with Vilanterol.
2,5-Dimethoxy-4-ethylamphetamine
The risk or severity of hypertension can be increased when 2,5-Dimethoxy-4-ethylamphetamine is combined with Vilanterol.
2,5-Dimethoxy-4-ethylthioamphetamine
The risk or severity of hypertension can be increased when Vilanterol is combined with 2,5-Dimethoxy-4-ethylthioamphetamine.
4-Bromo-2,5-dimethoxyamphetamine
The risk or severity of hypertension can be increased when 4-Bromo-2,5-dimethoxyamphetamine is combined with Vilanterol.
4-Methoxyamphetamine
The risk or severity of hypertension can be increased when 4-Methoxyamphetamine is combined with Vilanterol.
5-methoxy-N,N-dimethyltryptamine
The risk or severity of hypertension can be increased when Vilanterol is combined with 5-methoxy-N,N-dimethyltryptamine.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline
The risk or severity of adverse effects can be increased when 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline is combined with Vilanterol.
9-(N-methyl-L-isoleucine)-cyclosporin A
The risk or severity of adverse effects can be increased when Vilanterol is combined with 9-(N-methyl-L-isoleucine)-cyclosporin A.
Abacavir
Abacavir may decrease the excretion rate of Vilanterol which could result in a higher serum level.
Abatacept
The risk or severity of adverse effects can be increased when Abatacept is combined with Vilanterol.
Abediterol
The risk or severity of adverse effects can be increased when Vilanterol is combined with Abediterol.
Abetimus
The risk or severity of adverse effects can be increased when Abetimus is combined with Vilanterol.
Abexinostat
The risk or severity of QTc prolongation can be increased when Vilanterol is combined with Abexinostat.
Acarbose
Acarbose may decrease the excretion rate of Vilanterol which could result in a higher serum level.
Acebutolol
The therapeutic efficacy of Vilanterol can be decreased when used in combination with Acebutolol.
Aceclofenac
Aceclofenac may decrease the excretion rate of Vilanterol which could result in a higher serum level.
Acemetacin
Acemetacin may decrease the excretion rate of Vilanterol which could result in a higher serum level.
Acepromazine
The therapeutic efficacy of Vilanterol can be decreased when used in combination with Acepromazine.
Aceprometazine
The risk or severity of QTc prolongation can be increased when Vilanterol is combined with Aceprometazine.
2 References
  1. 1 . Harrell AW, Siederer SK, Bal J, Patel NH, Young GC, Felgate CC, Pearce SJ, Roberts AD, Beaumont C, Emmons AJ, Pereira AI, Kempsford RD: Metabolism and disposition of vilanterol, a long-acting beta(2)-adrenoceptor agonist for inhalation use in humans. Drug Metab Dispos. 2013 Jan;41(1):89-100. doi: 10.1124/dmd.112.048603. Epub 2012 Oct 4.PubMed: 23043183
  2. 2 . Spyratos D, Sichletidis L: Umeclidinium bromide/vilanterol combination in the treatment of chronic obstructive pulmonary disease: a review. Ther Clin Risk Manag. 2015 Mar 25;11:481-7. doi: 10.2147/TCRM.S67491. eCollection 2015.PubMed: 25848294