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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).
Inhaled therapeutics in chronic obstructive pulmonary disease
Published in Anthony J. Hickey, Heidi M. Mansour, Inhalation Aerosols, 2019
Tejas Sinha, Paul Dejulio, Philip Diaz
Long-acting beta agonist therapy has been an important component of COPD therapy since the 1980s; the modality of inhalational therapy has been critical to the success of LABA therapy, allowing targeted delivery to the lung and maximizing drug safety. LABA agents have numerous clinical benefits, including reducing acute exacerbations of disease, improving airflow, and decreasing dyspnea (18,41,42). LABA agents have been utilized for monotherapy, but there are also known synergistic benefits when they are utilized as combination agents with LAMAs and ICSs (43,44). Formoterol and salmeterol are two of the oldest and most common agents utilized. More recently, very long-acting beta agonists (VLABAs) have become available (45). Such agents are available for once daily dosing and include indacaterol, vilanterol, and olodaterol (45–47).
Globally Optimal Adaptive Trial Designs
Published in Mark Chang, John Balser, Jim Roach, Robin Bliss, Innovative Strategies, Statistical Solutions and Simulations for Modern Clinical Trials, 2019
Mark Chang, John Balser, Jim Roach, Robin Bliss
Indacaterol was an investigational, novel, inhaled once-daily ultra-long-acting β2—agonist for the treatment of COPD. Indacaterol was a small new molecular entity (NME, Figure 4.7) brought into clinical development around 2005, with the following profiles.
The safety of indacaterol for the treatment of COPD
Published in Expert Opinion on Drug Safety, 2018
Evgenios I. Metaxas, Evangelos Balis
Based on the efficacy studies, indacaterol has been approved for use in patients with COPD. The only contra-indication is hypersensitivity to the active substance or to any of the excipients. The approved doses range from 75 to 300 μg and is formulated as inhalation powder hard capsules delivered using a dry-powder inhaler. Indacaterol was first approved in the European Union in 2009 by the European Medicines Agency (EMA) as a once-daily treatment at doses of 150 and 300 μg. The US Food and Drug Administration (FDA) approved indacaterol at a lower dose of 75 μg once daily in 2011.
The effects of asthma medications on reactive oxygen species production in human monocytes
Published in Journal of Asthma, 2018
Ming-Kai Tsai, Yi-Ching Lin, Ming-Yii Huang, Min-Sheng Lee, Chang-Hung Kuo, Po-Lin Kuo, Ching-Hsiung Lin, Chih-Hsing Hung
Asthma medications reduce airway inflammation and relief asthma symptoms. Leukotriene modifiers, long-acting β2-adrenoreceptor agonists (LABAs), and inhaled corticosteroids (ICSs) are common long-term asthma control medications. Leukotriene receptor antagonists (LTRA), such as montelukast, would prevent provoking asthma responses, ameliorate asthma symptoms, improve lung function, and reduce β2-agonist use in patients with persistent asthma [5, 6]. β2 adrenoceptor agonists are used widely as bronchodilators in treatment of asthma and have important anti-inflammatory effects on eosinophils and neutrophils [7, 8]. Formoterol and salmeterol are two inhaled long-acting β2-adreno-receptor agonists (LABAs) widely used for the treatment of asthma and chronic obstructive pulmonary disease (COPD). These two common LABAs were reported to have inhibitory effects on the expression of pro-inflammatory cytokines. Formoterol could suppress lipopolysaccharide (LPS)-induced IL-6 expression in a mouse model [9]. Salmeterol could suppress LPS-induced TNF-α production in THP-1 cells [10] and it also reduces the IgE-dependent TNF-α production in human skin mast cells [11]. Indacaterol, an extra-LABA, is new breakthrough for LABA and can be a monotherapy for COPD, but not for asthma. Indacaterol is able to induce a rapid and long-lasting relaxation of airway smooth muscles via a prolonged activation of β2-receptors, and provides a persistent bronchodilation due to the prolonged competitive blockade of M3 muscarinic receptors [12, 13]. ICS is known to be effective as a maintenance medication in persistent asthma. The clinical usefulness of fixed-dose maintenance therapy with ICS/LABA combination inhalers, such as fluticasone/salmeterol and budesonide/formoterol, has been established though the long-term anti-inflammatory effects of these two inhalers are limited [14].
State-of-the-art beta-adrenoreceptor agonists for the treatment of asthma
Published in Expert Opinion on Pharmacotherapy, 2022
W. Tatiana Garzon-Siatoya, Ismael Carrillo-Martin, Sergio E Chiarella, Alexei Gonzalez-Estrada
Indacaterol is an ultra-long-acting β2-AR agonist and the first inhaled bronchodilator in this category. In vitro and in vivo studies show that indacaterol has a rapid onset of action, bronchodilation for at least 24 hours, and an optimal safety profile [47]. In addition, it is a potent, lipophilic drug with an intrinsic efficacy that has been shown to influence several aspects of its pharmacokinetic profile in vitro [48].