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Salbutamol

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https://www.readbyqxmd.com/read/28932468/crystal-structure-of-rac-4-2-tert-butyl-aza-nium-yl-1-hy-droxy-eth-yl-2-hy-droxy-meth-yl-phenol-benzoate
#1
Wenju Liu, Qiliang Chen, Linda Yu
The title salt, C13H22NO3(+)·C7H5O2(-), comprises one salbutamol cation {sys-tematic name: 4-[2-(tert-butyl-aza-nium-yl)-1-hy-droxy-eth-yl]-2-(hy-droxy-meth-yl)phenol} and a benzoate anion. The cation shows disorder of the hy-droxy group [occupancy ratio 0.738 (3):0.262 (3)] at the stereogenic C atom. The non-planar benzoate anion [the dihedral angle between the benzene ring and the carboxyl group is 11.30 (8)°] is linked to the salbutamol cation by a medium-strength O-H⋯O hydrogen bond. Other inter-molecular O-H⋯O and N-H⋯O hydrogen bonds of weaker nature give rise to [001] chains...
September 1, 2017: Acta Crystallographica. Section E, Crystallographic Communications
https://www.readbyqxmd.com/read/28913547/probucol-prevents-the-attenuation-of-%C3%AE-2-adrenoceptor-mediated-vasodilation-of-retinal-arterioles-in-diabetic-rats
#2
Asami Mori, Kentaro Higashi, Shun Wakao, Kenji Sakamoto, Kunio Ishii, Tsutomu Nakahara
Probucol is an antihyperlipidemic drug with potent antioxidant properties. Oxidative stress plays an important role in the pathogenesis of diabetic retinopathy. In this study, we aimed to investigate the protective effects of probucol against diabetes-induced retinal vascular dysfunction in a rat model of diabetes. Diabetes was induced by a combination of streptozotocin treatment and D-glucose feeding, and retinal vasodilator responses were assessed by measuring the diameter of retinal arterioles. The vasodilator effect of salbutamol, a β2-adrenoceptor agonist, on retinal arterioles was significantly diminished 2 weeks after the induction of diabetes...
September 14, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28901297/metabolic-effects-of-inhaled-salbutamol-determined-by-exhaled-breath-analysis
#3
Martin T Gaugg, Anna Engler, Yvonne Nussbaumer-Ochsner, Lukas Bregy, Anna S Stöberl, Thomas Gaisl, Tobias Bruderer, Renato Zenobi, Malcolm Kohler, Pablo Martinez-Lozano Sinues
We explore whether real-time breath analysis by high resolution mass spectrometry is suitable to monitor changes at the metabolic level due to inhaling bronchodilator medication. We compared the breath levels of metabolites in a group of patients (n = 50) at baseline and 10 and 30 min after inhalation of 200 μg salbutamol. The same procedure was performed with a group of controls (n = 48) inhaling a placebo spray. A total of 131 mass spectral features were significantly altered as a result of inhaling medication, but not after inhaling placebo...
September 13, 2017: Journal of Breath Research
https://www.readbyqxmd.com/read/28886711/structure-and-functional-impact-of-seed-region-variant-in-mir-499-gene-family-in-bronchial-asthma
#4
Eman A Toraih, Mohammad H Hussein, Essam Al Ageeli, Eman Riad, Nouran B AbdAllah, Ghada M Helal, Manal S Fawzy
BACKGROUND: Small non-coding RNAs (microRNAs) have been evolved to master numerous cellular processes. Genetic variants within microRNA seed region might influence microRNA biogenesis and function. The study aimed at determining the role of microRNA-499 (MIR-499) gene family polymorphism as a marker for susceptibility and progression of bronchial asthma and to analyze the structural and functional impact of rs3746444 within the seed region. METHODS: Genotyping for 192 participants (96 patients and 96 controls) in the discovery phase and 319 subjects (115 patients and 204 controls) in the replication phase was performed via Real Time-Polymerase Chain Reaction technology...
September 8, 2017: Respiratory Research
https://www.readbyqxmd.com/read/28882385/lung-deposition-and-systemic-bioavailability-of-different-aerosol-devices-with-and-without-humidification-in-mechanically-ventilated-patients
#5
Islam O F Moustafa, Mohammed R A-A Ali, Moataz Al Hallag, Hoda Rabea, James B Fink, Patricia Dailey, Mohamed E A Abdelrahim
BACKGROUND: During mechanical ventilation medical aerosol delivery has been reported to be upto two fold greater with dry inhaled gas than with heated humidity. Urine levels at 0.5 h post dose (URSAL0.5%) has been confirmed as an index of lung deposition and 24 h (URSAL24%) as index of systemic absorption. Our aim was to determine the effect of humidification and aerosol device type on drug delivery to ventilated patients using urine levels. METHODS: In a randomized crossover design, 36 (18female) mechanically ventilated patients were assigned to one of three groups...
September 4, 2017: Heart & Lung: the Journal of Critical Care
https://www.readbyqxmd.com/read/28875855/impurity-profile-of-bronchodilators-used-in-asthma-a-critical-review
#6
Krunal J Prajapati, Charmy Kothari
BACKGROUND: Asthma is defined as a heterogeneous disease usually characterized by chronic airway inflammation (GINA 2016) affecting almost 334 million people worldwide (Global asthma report 2014). Treatment of asthma with a long-acting bronchodilator is important because it reduces the symptoms that occur at night or in the early morning and it is very effective to use as a long term control medication for asthma by preventing asthmatic symptoms. The main objective of this review is to describe the impurity profile and force degradation studies for three major classes of bronchodilators namely β2-adrenoceptor agonists, muscarinic receptor antagonists and xanthine...
August 29, 2017: Current Drug Discovery Technologies
https://www.readbyqxmd.com/read/28875453/laboratory-study-comparing-pharmacopeial-testing-of-nebulizers-with-evaluation-based-on-nephele-mixing-inlet-methodology
#7
Mårten Svensson, Elna Berg, Jolyon Mitchell, Dennis Sandell
Determination of fine droplet dose with preparations for nebulization, currently deemed to be the metric most indicative of lung deposition and thus in vivo responses, involves combining two procedures following practice as described in the United States Pharmacopeia and the European Pharmacopeia. Delivered dose (DD) is established by simulating tidal breathing at the nebulizer, collecting the medication on a filter downstream of the nebulizer mouthpiece/facemask. Fine droplet fraction (FDF<x μm) is determined separately using a cooled cascade impactor operated at 15 L/min...
September 5, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28860381/%C3%AE-2-adrenoreceptor-is-a-regulator-of-the-%C3%AE-synuclein-gene-driving-risk-of-parkinson-s-disease
#8
Shuchi Mittal, Kjetil Bjørnevik, Doo Soon Im, Adrian Flierl, Xianjun Dong, Joseph J Locascio, Kristine M Abo, Elizabeth Long, Ming Jin, Bing Xu, Yang K Xiang, Jean-Christophe Rochet, Anders Engeland, Patrizia Rizzu, Peter Heutink, Tim Bartels, Dennis J Selkoe, Barbara J Caldarone, Marcie A Glicksman, Vikram Khurana, Birgitt Schüle, David S Park, Trond Riise, Clemens R Scherzer
Copy number mutations implicate excess production of α-synuclein as a possibly causative factor in Parkinson's disease (PD). Using an unbiased screen targeting endogenous gene expression, we discovered that the β2-adrenoreceptor (β2AR) is a regulator of the α-synuclein gene (SNCA). β2AR ligands modulate SNCA transcription through histone 3 lysine 27 acetylation of its promoter and enhancers. Over 11 years of follow-up in 4 million Norwegians, the β2AR agonist salbutamol, a brain-penetrant asthma medication, was associated with reduced risk of developing PD (rate ratio, 0...
September 1, 2017: Science
https://www.readbyqxmd.com/read/28839497/bronchodilator-response-assessment-of-the-small-airways-obstructive-pattern
#9
Plamen Bokov, Clémence Martin, Sémia Graba, Karine Gillet-Juvin, Mohamed Essalhi, Christophe Delclaux
BACKGROUND: A concomitant decrease in FEV1 and FVC with normal FEV1/FVC ratio and TLC defines small airways obstructive pattern (SAOP) and constitutes a classic pitfall of pulmonary-function-tests interpretation. OBJECTIVE: To evaluate the prevalence of flow- (FEV1 increase≥12% and 200 mL), volume- (FVC or inspiratory capacity [IC] increase≥12% and 200 mL), flow and volume-, and non-response to bronchodilation in patients with SAOP. An additional objective was to assess whether impulse oscillometry (IOS) parameters allow the diagnosis of SAOP and its reversibility...
2017: Open Respiratory Medicine Journal
https://www.readbyqxmd.com/read/28835457/neuroendocrine-modulation-of-il-27-in-macrophages
#10
Julian Roewe, Maximilian Higer, Dennis R Riehl, Adrian Gericke, Markus P Radsak, Markus Bosmann
Heterodimeric IL-27 (p28/EBV-induced gene 3) is an important member of the IL-6/IL-12 cytokine family. IL-27 is predominantly synthesized by mononuclear phagocytes and exerts immunoregulatory functional activities on lymphocytic and nonlymphocytic cells during infection, autoimmunity or neoplasms. There is a great body of evidence on the bidirectional interplay between the autonomic nervous system and immune responses during inflammatory disorders, but so far IL-27 has not been defined as a part of these multifaceted neuroendocrine networks...
August 23, 2017: Journal of Immunology: Official Journal of the American Association of Immunologists
https://www.readbyqxmd.com/read/28834381/small-airway-oscillometry-indices-repeatability-and-bronchodilator-responsiveness-in-young-children
#11
Hanna Knihtilä, Anne Kotaniemi-Syrjänen, Anna S Pelkonen, Satu Kalliola, Mika J Mäkelä, Leo Pekka Malmberg
INTRODUCTION: The impulse oscillometry (IOS) indices absolute and relative difference between respiratory resistance at 5 and 20 Hz (R5-20 and R5-20%, respectively) and the area under the reactance curve (AX) are postulated to reflect small airway function. Data on their cutoff values to evaluate bronchodilator responsiveness (BDR) or between-visit changes after interventions are limited in young children. METHODS: We evaluated the BDR of 103 healthy children aged 2-7 years, who received either salbutamol (n = 84) or placebo (n = 19) in order to determine cutoff values for BDR of R5-20, R5-20%, and AX...
August 18, 2017: Pediatric Pulmonology
https://www.readbyqxmd.com/read/28831247/validity-of-physician-diagnosed-copd-in-relation-to-spirometric-definitions-of-copd-in-a-general-population-aged-50-64-years-the-scapis-pilot-study
#12
Kjell Torén, Nicola Murgia, Anna-Carin Olin, Jan Hedner, John Brandberg, Annika Rosengren, Göran Bergström
BACKGROUND: In epidemiological studies, items about physician-diagnosed COPD are often used. There is a lack of validation and standardization of these items. MATERIALS AND METHODS: In a general population-based study, 1,050 subjects completed a questionnaire and performed spirometry, including forced expiratory volume in 1 second (FEV1) and forced vital capacity (FVC) after inhalation of 400 µg of salbutamol. COPD was defined as the ratio of FEV1/FVC <0.7 after bronchodilation...
2017: International Journal of Chronic Obstructive Pulmonary Disease
https://www.readbyqxmd.com/read/28814783/mycoplasma-pneumoniae-associated-bronchiolitis-obliterans-following-acute-bronchiolitis
#13
Chengsong Zhao, Jinrong Liu, Haiming Yang, Li Xiang, Shunying Zhao
The characteristics of Mycoplasma pneumonia (M. pneumoniae)-associated bronchiolitis obliterans (BO) are not well known. We retrospectively reviewed 17 patients with M. pneumoniae-associated BO. All patients had M. pneumoniae-associated acute bronchiolitis prior to the development of BO. In the acute bronchiolitis stage, all patients had fever and cough; six patients also had wheezing and dyspnoea. BO was diagnosed approximately 1.5-8 months later based on clinical manifestations and chest high-resolution computed tomography (HRCT) findings...
August 16, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28759088/the-effects-of-treatment-in-patients-with-childhood-asthma-on-the-elastic-properties-of-the-aorta
#14
Osman Bektaş, Zeki Yüksel Günaydin, Ahmet Karagöz, Recep Akgedik, Adil Bayramoğlu, Ahmet Kaya
INTRODUCTION: The study aimed to investigate the effects of treatment in patients with childhood asthma on the elastic properties of the aorta and cardiovascular risk. METHODS: The study was performed in 66 paediatric patients diagnosed with bronchial asthma (BA). All patients were administered the β2 agonist, salbutamol, for seven days, followed by one month of montelukast and six months of inhaled steroid treatment. All patients underwent conventional transthoracic echocardiographic imaging before and after treatment...
May 2017: Cardiovascular Journal of Africa
https://www.readbyqxmd.com/read/28732286/development-of-liquid-chromatographic-methods-for-enantioseparation-and-sensitive-detection-of-%C3%AE-adrenolytics-%C3%AE-2-agonists-in-human-plasma-using-a-single-enantiomer-reagent
#15
Poonam Malik, Ravi Bhushan
Enantioseparation of four commonly used β-adrenolytics (bisoprolol, salbutamol, and carvedilol, marketed as racemic mixtures) has been achieved by both TLC and RPHPLC via an indirect approach. A new chiral reagent, (S)-naproxen benzotriazole ester, was synthesized and it was characterized by UV, IR, (1)HNMR, elemental analysis and polarimetry. It was used to synthesize diastereomeric derivatives of the three β-adrenolytics under microwave irradiation. TLC separation of diastereomeric derivatives was achieved which were then isolated by preparative approach; these were characterized and were used as standard reference for determining absolute configuration of diastereomeric derivatives and for establishing validated HPLC method for enantioseparation and sensitive detection of the three β-adrenolytics in human plasma...
September 1, 2017: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/28724273/effects-of-inhaled-salbutamol-on-sport-specific-fitness-of-non-asthmatic-football-players
#16
Farzin Halabchi, Mahdi Abarashi, Mohammad Ali Mansournia, Tohid Seifbarghi
In this article, we investigated the effectiveness of inhaled salbutamol withtherapeutic dose on the sport-specific performance of non-asthmatic young football players. In a double-blinded, randomised placebo controlled trial with 2-treatment, 2-period crossover design, twenty participants who were non-asthmatic junior professional football players were randomly allocated to two groups. Fifteen minutes before sport-specific fitness testing, each group randomly received 2 inhalations (200 micrograms) of salbutamol or placebo, respectively...
May 2017: Acta Medica Iranica
https://www.readbyqxmd.com/read/28723410/innovative-pmdi-formulations-of-spray-dried-nanoparticles-for-efficient-pulmonary-drug-delivery
#17
Hao-Ying Li, En-Yu Xu
For drug delivery to the lungs, the aerodynamic size of drug particles plays a predominant role in determining the sites of deposition in the airway, and the particles with the size less than 2μm are highly expected as they will be preferably delivered to the ideal site of alveolar regions. In this paper, a novel platform technology has been developed, where the water (containing pharmaceutically active agents)-in-oil (w/o) microemulsions were spray-dried to generate nanosized drug particles that were able to be homogeneously dispersed in the propellant to form an exceptionally stable suspensions with no precipitates or flocculates during a long time storage...
July 16, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28719816/sulfate-radical-induced-degradation-of-%C3%AE-2-adrenoceptor-agonists-salbutamol-and-terbutaline-phenoxyl-radical-dependent-mechanisms
#18
Lei Zhou, Mohamad Sleiman, Corinne Ferronato, Jean-Marc Chovelon, Pascal de Sainte-Claire, Claire Richard
The present study investigated the reactivity and oxidation mechanisms of salbutamol (SAL) and terbutaline (TBL), two typical β2-adrenoceptor agonists, towards sulfate radical (SO4(-)) by using photo-activated persulfate (PS). The reaction pathways and mechanisms were proposed based on products identification using high resolution HPLC-ESI-MS, laser flash photolysis (LFP) and molecular orbital calculations. The results indicated that SO4(-) was the dominant reactive species in the UV/PS process. The second-order rate constants of sulfate radical reaction with SAL and TBL were measured as (3...
July 14, 2017: Water Research
https://www.readbyqxmd.com/read/28718249/frequency-of-undiagnosed-chronic-obstructive-pulmonary-disease-in-patients-with-coronary-artery-disease
#19
Raza Ullah, Shahid Salam, Tahir Ghaffar, Rahim Muhammad, Imran Khan
BACKGROUND: Chronic obstructive airway disease (COPD) is considered as risk factor for coronary artery disease (CAD) along with other risk factors. This study was conducted to determine the frequency of undiagnosed chronic obstructive pulmonary disease in patients with coronary artery disease. METHODS: This cross-sectional study was conducted in the Pulmonology and Cardiology wards/OPD's of Khyber Teaching Hospital Peshawar. Patients more than 35 years of age, diagnosed with CAD of either gender were included...
April 2017: Journal of Ayub Medical College, Abbottabad: JAMC
https://www.readbyqxmd.com/read/28710850/efficacy-and-safety-of-beclomethasone-dipropionate-breath-actuated-or-metered-dose-inhaler-in-pediatric-patients-with-asthma
#20
Mark Vandewalker, Lisa Hickey, Calvin J Small
BACKGROUND: Breath-actuated inhalers (BAI) eliminate the need for hand-breath coordination and, therefore, simplify the delivery of inhaled medication. OBJECTIVE: To evaluate the efficacy and safety of beclomethasone dipropionate BAI and metered-dose inhaler (MDI) versus placebo in pediatric patients ages 4-11 years with persistent asthma. METHODS: In this double-blind, double-dummy, phase III study, 628 children with persistent asthma were randomly assigned (1:1:1:1:1) to twice-daily beclomethasone dipropionate (BAI 80 μg/day, BAI 160 μg/day, MDI 80 μg/day, or MDI 160 μg/day) or to placebo...
September 14, 2017: Allergy and Asthma Proceedings:
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