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Adrenergic Agonists
Published in Sahab Uddin, Rashid Mamunur, Advances in Neuropharmacology, 2020
Other long-acting β2 receptor selective agonists are salmeterol, formoterol, arformoterol, carmoterol, and indacaterol. Salmeterol is a β2 selective receptor agonist, highly specific and showing long duration of activity which is more than 12 h. It is mainly used for treating COPD. It is metabolized by CYP3A4. The onset of activity is slow. Formoterol β2 receptor selective agonist with quick action while used as an inhalation and a duration of action which is long and lasts for 12 h. The drug is used in treating bronchospasm, asthma, and obstructive pulmonary disease. Arformoterol is a long-acting β2 receptor selective agonist. The drug is used long-term for treating COPD and bronchoconstriction. Metabolism is by the enzymes CYP2C19 and CYP2D6. The adverse events include insomnia, tachycardia, reduction in plasma potassium level and a rise in the level of plasma glucose. Carmoterol, a β2 selective adrenergic agonist is having greater selectivity. The drug shows a fast onset of activity and the duration of activity is very long which lasts more than 24 h. It is a bronchodilator used in treating asthma and COPD. Indacaterol is a β2 adrenergic receptor selective agonist with a rapid onset and long duration in activity. The drug is used in treating COPD and asthma (Brunton et al., 2011; Barisione et al., 2010).
Nebulizers
Published in Anthony J. Hickey, Sandro R.P. da Rocha, Pharmaceutical Inhalation Aerosol Technology, 2019
John N. Pritchard, Dirk von Hollen, Ross H.M. Hatley
The exception to this are the long-acting beta2-agonists formoterol and arformoterol available in the United States, in contrast to this, at the time of writing there were around 27 long-acting drugs or drug combinations in late stage development or recently launched in inhaler form for the treatment of asthma and COPD. Long-acting formulations decrease the burden of disease upon the patient, adherence is improved with once daily medication compared with 2 times, 3 times, or 4 times a day (Falagas et al. 2015) and the likelihood of readmission is reduced (Bollu et al. 2013). Therefore, the lack of nebulized options for the treatment of the sickest asthma and COPD patients who may struggle with correct use of inhalers is unlikely to persist in the competitive market of inhaled therapy. There are signs that the development of handheld mesh nebulizers, with most of the convenience of inhalers and additional benefits of adherence monitoring, is resulting in the development of many new drug formulations in nebulized form (Santus et al. 2017, Quinn et al. 2018). For example, Sunovion recently received approval in the United States for their nebulized long-acting muscarinic.
Current pharmacogenomic recommendations in chronic respiratory diseases: Is there a biomarker ready for clinical implementation?
Published in Expert Review of Respiratory Medicine, 2022
Ingrid Fricke-Galindo, Ramcés Falfán-Valencia
Arformoterol is an (R,R) enantiomer of formoterol [21]. Both drugs are nebulized long-acting β-agonists (LABA) prescribed in COPD [22], although arformoterol has been reported to be more potent than formoterol owing to its greater affinity for the β2-adrenergic receptor [21]. Due to their metabolic pathways, the pharmacogenomic information included in the approved labels is focused on the UGT1A1, CYP2D6, and CYP2C19 genes. Apparently, for arformoterol, the pharmacogenetic variants do not affect the systemic exposure to the drug; meanwhile, there is a lack of studies on the pharmacogenetics of formoterol. There are no reports about studying these or other enzymes in the pharmacogenetics of formoterol and arformoterol. On the contrary, the studies found in the scientific literature comprise the evaluation of ADRB2 genetic variants in the combined therapy, including formoterol, but these have reported controversial results [23–26].
Pharmacogenomics of chronic obstructive pulmonary disease
Published in Expert Review of Respiratory Medicine, 2019
The U.S. Food and Drug Administration (FDA) maintains a list of drugs with pharmacogenetics biomarkers included in the drug label [101]. The majority of this list includes anti-cancer therapies, though several medications relevant to COPD are included. The labels for several bronchodilators, including arformoterol, formoterol, indacaterol, and umeclidinium, mention pharmacogenetic variants related to their clinical pharmacology; however, none of these variants is felt to be clinically-relevant.
Emergency management of chlorine gas exposure – a systematic review
Published in Clinical Toxicology, 2019
Alice Huynh Tuong, Thomas Despréaux, Thomas Loeb, Jérôme Salomon, Bruno Mégarbane, Alexis Descatha
In contrast, similar experiments with intranasal instillation of arformoterol 10 ng/20 g, a ß2-agonist, resulted in a significant decrease in airway resistance within one day, had positive effects on elastance at the sixth day post-exposure, but did not alter significantly the number of BAL cells and protein concentration [50].