Search results for "adrenergic beta-2 receptor agonists"

Salmeterol Xinafoate (SX) loaded into mucoadhesive solid lipid microparticles for COPD treatment

2019

Chronic obstructive pulmonary disease (COPD) is one of the main health problems worldwide. It is characterised by chronic inflammation in the lungs that leads to progressive, chronic, largely irreversible airflow obstruction. The use of long-acting β agonists remain today the frontline treatment for COPD with the aim of minimizing side effects and enhancing therapeutic usefulness. To this purpose, in this paper, mucoadhesive solid lipid microparticles (SLMs) containing a long-acting β-2 agonist, Salmeterol Xinafoate (SX) were prepared, characterised (size, z-potential, aerodynamic diameter, turbidimetric evaluations, drug loading and entrapping efficiency) and tested in a model of bronchial…

Symptom variability and control in COPD: Advantages of dual bronchodilation therapy

2017

Abstract Background Chronic obstructive pulmonary disease (COPD) is a heterogeneous disorder characterized by usually progressive development of airflow obstruction that is not fully reversible. While most patients will experience symptoms throughout the day or in the morning upon awakening, many patients do not experience their symptoms as constant but report variability in symptoms during the course of the day or over time. Symptom variability adversely affects patients' health status and increases the risk of COPD exacerbations. Methods We examined data from the literature on symptom variability and control in patients with COPD, with focus on the use of inhaled bronchodilator therapy wi…

Early management of COPD: Where are we now and where do we go from here? a delphi consensus project

2019

Fabiano Di Marco,1 Piero Balbo,2 Francesco de Blasio,3 Vittorio Cardaci,4 Nunzio Crimi,5 Giuseppe Girbino,6 Girolamo Pelaia,7 Pietro Pirina,8 Pietro Roversi,9 Pierachille Santus,10,11 Nicola Scichilone,12 Alessandro Vatrella,13 Patrizio Pasqualetti,14 Mauro Carone15 1Department of Health Sciences, University of Milan, Respiratory Unit, Papa Giovanni XXIII Hospital, Bergamo, Italy; 2SC Malattie dell’Apparato Respiratorio, AOU Maggiore della Carità, Novara, Italy; 3Respiratory Medicine and Pulmonary Rehabilitation Section, Clinic Center S.p.A. Private Hospital, Department of Medicine and Health Sciences “V Tiberio”, University of Molise, Campobasso, It…

Reslizumab as add-on therapy in patients with refractory asthma

2020

### Key messages #### What is the key question? #### What is the bottom line? #### Why read on? Asthma is a common disease, affecting an estimated 334 million people worldwide, with considerable impact on quality of life and high associated costs.1–3 Asthma severity is assessed retrospectively from the level of treatment required to control symptoms and exacerbations. Approximately 5%–10% of patients with asthma are believed to suffer from severe disease.4 Patients with severe asthma typically require ongoing maintenance therapy with high-dose inhaled corticosteroid (ICS)/long-acting beta-agonist (LABA).2 Furthermore, systemic corticosteroids (SCS) are often required for potentially life-th…

Synthesis and pharmacological characterization of beta2-adrenergic agonist enantiomers: zilpaterol.

2009

The beta-adrenergic agonist 1 (zilpaterol) is used as production enhancer in cattle. Binding experiments of separated enantiomers on recombinant human beta(2)-adrenergic and mu-opioid receptors and functional studies showed that the (-)-1 enantiomer accounts for essentially all the beta(2)-adrenergic agonist activity and that it exhibits less affinity toward the mu-opioid receptor than (+)-1, which is a mu-opioid receptor antagonist. X-ray crystallography revealed the absolute configuration of (-)-1 to be 6R,7R.

The Arg/Arg polymorphism of the ADRB2 is associated with the severity of allergic asthma

2016

Differences in the efficacy and safety among inhaled corticosteroids (ICS)/long-acting beta2-agonists (LABA) combinations in the treatment of chronic…

2015

Inhaled corticosteroids (ICS) are frequently recommended for the treatment of asthma and COPD, often in combination with long-acting beta2-agonists (LABA), depending on the severity of the disease and/or on the specific phenotype. Several ICS/LABA combinations are currently available that differ in their pharmacokinetic characteristics and dose of both components. Thus, this review assesses differences in the efficacy and the safety profiles of the ICS components in the two more frequently used ICS/LABA combinations (budesonide/formoterol and fluticasone/salmeterol) for the management of COPD. Whereas the basic mechanism of action is similar for all ICS (binding with the intracellular gluco…

Th17 immunity in children with allergic asthma and rhinitis: a pharmacological approach

2013

Th17 cells and IL-17A play a role in the development and progression of allergic diseases. We analyzed the IL-17A levels in sputum supernatants (Ss), nasal wash (NW) and plasma (P) from Healthy Controls (HC) and children with Asthma/Rhinitis. We tested the expression of IL-17A, RORγ(t) and FOXP3 in peripheral blood T-lymphocytes from intermittent and mild-moderate asthma. The effect of Budesonide and Formoterol was tested "in vitro" on IL-17A, RORγ(t) and FOXP3 expression in cultured T-lymphocytes from mild-moderate asthma/persistent rhinitis patients, and on nasal and bronchial epithelial cells stimulated with NW and Ss from mild-moderate asthma/persistent rhinitis. Further, the effect of …

LABA/LAMA fixed-dose combinations in patients with COPD: A systematic review

2018

Paola Rogliani,1 Luigino Calzetta,1 Fulvio Braido,2 Mario Cazzola,1 Enrico Clini,3 Girolamo Pelaia,4 Andrea Rossi,5 Nicola Scichilone,6 Fabiano Di Marco7 1Department of Experimental Medicine and Surgery, University of Rome Tor Vergata, Rome, Italy; 2Department of Internal Medicine, IRCCS San Martino Genoa University Hospital, Genoa, Italy; 3Department of Medical and Surgical Sciences, University of Modena and Reggio Emilia, Modena, Italy; 4Department of Medical and Surgical Sciences, Section of Respiratory Diseases, Magna Græcia University, Catanzaro, Italy; 5Pulmonary Unit, University of Verona, Verona, Italy; 6Department of Internal Medicine, University of Palermo, Palermo, Italy; 7…

The human near-term myometrial beta 3-adrenoceptor but not the beta 2-adrenoceptor is resistant to desensitisation after sustained agonist stimulatio…

2004

International audience; 1. In order to compare the beta(2)- and beta(3)-adrenoceptor (beta-AR) desensitisation process in human near-term myometrium, we examined the influence of a pretreatment of myometrial strips with either a beta(2)- or a beta(3)-AR agonist (salbutamol or SR 59119A, respectively, both at 10 microm, for 5 and 15 h) on the relaxation and the cyclic adenosine monophosphate (cAMP) production induced by these agonists. 2. To assess some of the mechanisms potentially implicated in the beta-AR desensitisation process, we studied the influence of such treatment on the number of beta(2)- and beta(3)-AR binding sites, the beta(2)- and beta(3)-AR transcripts expression and the pho…