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Beta agonists

Syed Rizwan A Bokhari, Faisal Akhtar, Qurrat-Ul-Ain Abid, Uzma Jahanzaib, Maria R Bokhari, Sana Hasan, Khurshid Khan
Postural hypotension, as a manifestation of autonomic neuropathy is a very sinister long-term debilitating complication of diabetes, is usually irreversible and tough to manage with medications. The treatment of this condition following the standard treatment protocols can be contraindicated in the patients with underlying heart conditions. We report the case of a patient at our hospital who presented with full-blown symptomatic dysautonomia secondary to long-standing diabetes, with bedside testing positive for autonomic dysfunction...
January 8, 2018: Curēus
Sheryl Magzamen, Assaf P Oron, Emily R Locke, Vincent S Fan
BACKGROUND: Studies have linked ambient air pollution to chronic obstructive pulmonary disease (COPD) healthcare encounters. However, the association between air quality and rescue medication use is unknown. OBJECTIVES: We assessed the role of air pollution exposure for increased short-acting beta-2-agonist (SABA) use in patients with COPD through use of remote monitoring technology. METHODS: Participants received a portable electronic inhaler sensor to record the date, time and location for SABA use over a 3-month period...
March 13, 2018: Occupational and Environmental Medicine
Marsha A Raebel, Susan M Shetterly, Glenn K Goodrich, Courtney B Anderson, Jo Ann Shoup, Nicole Wagner, Bruce G Bender
No abstract text is available yet for this article.
March 12, 2018: Journal of General Internal Medicine
Tom Podewin, Julia Ast, Johannes Broichhagen, Nicholas H F Fine, Daniela Nasteska, Philipp Leippe, Manuel Gailer, Teresa Buenaventura, Nisha Kanda, Ben J Jones, Celine M'Kadmi, Jean-Louis Baneres, Jacky Marie, Alejandra Tomas, Dirk Trauner, Anja Hoffmann-Röder, David J Hodson
Understanding the activation and internalization of G protein-coupled receptors (GPCRs) using conditional approaches is paramount to developing new therapeutic strategies. Here, we describe the design, synthesis, and testing of ExONatide , a benzylguanine-linked peptide agonist of the glucagon-like peptide-1 receptor (GLP-1R), a class B GPCR required for maintenance of glucose levels in humans. ExONatide covalently binds to SNAP-tagged GLP-1R-expressing cells, leading to prolonged cAMP generation, Ca2+ rises, and intracellular retention of the receptor...
February 28, 2018: ACS Central Science
João Cavaleiro Rufo, Inês Paciência, Diana Silva, Carla Martins, Joana Madureira, Eduardo de Oliveira Fernandes, Patrícia Padrão, Pedro Moreira, Luís Delgado, André Moreira
BACKGROUND: Endurance swimming exercises coupled to disinfection by-products exposure has been associated with increased airways dysfunction and neurogenic inflammation in elite swimmers. However, the impact of swimming pool exposure at a recreational level on autonomic activity has never been explored. Therefore, this study aimed to investigate how swimming pool attendance is influencing lung and autonomic function in school-aged children. METHODS: A total of 858 children enrolled a cross sectional survey...
2018: PloS One
Matthew Morten, Adam Collison, Vanessa E Murphy, Daniel Barker, Christopher Oldmeadow, John Attia, Joseph Meredith, Heather Powell, Paul D Robinson, Peter D Sly, Peter G Gibson, Joerg Mattes
BACKGROUND: The single-centre double-blind, randomised controlled Managing Asthma in Pregnancy (MAP) trial in Newcastle, Australia, compared a treatment algorithm using the fraction of exhaled nitric oxide (FeNO) in combination with asthma symptoms (FeNO group) against a treatment algorithm using clinical symptoms only (clinical group) in pregnant asthmatic women (ANZ Clinical Trials Registry, number 12607000561482). The primary outcome was a 50% reduction in asthma exacerbations during pregnancy in the FeNO group...
March 7, 2018: Journal of Allergy and Clinical Immunology
Kerry R Belton, Yuan Tian, Limin Zhang, Mallappa Anitha, Philip B Smith, Gary H Perdew, Andrew D Patterson
The liver and the mammary gland have complementary metabolic roles during lactation. Substrates (e.g., glucose and amino acids) synthesized by the liver are released into the circulation and are taken up by the mammary gland for milk production (e.g., lactose and the glycerol backbone of milk triglycerides). The aryl hydrocarbon receptor (AHR) has been identified as a lactation regulator in mice, and its activation has been associated with myriad morphological, molecular, and functional defects such as stunted gland development, decreased milk production, and changes in gene expression...
March 9, 2018: Journal of Proteome Research
Zobair M Younossi, Maria Stepanova, Harry L A Janssen, Kosh Agarwal, Mindie H Nguyen, Ed Gane, Naoky Tsai, Issah Younossi, Andrei Racila
BACKGROUND AND AIM: Chronic infection with hepatitis B virus (HBV) causes liver disease and cirrhosis. It is not clear how treatment of chronic HBV infection affects patient-reported outcomes (PROs). We aimed to assess changes in PROs in patients treated for chronic HBV infection. METHODS: We collected and analyzed PRO data from 242 patients with chronic HBV infection (without advanced fibrosis or cirrhosis) enrolled in 2 international phase 2 blinded controlled clinical trials from 2015 through 2017...
March 2, 2018: Clinical Gastroenterology and Hepatology
Guillaume Chaussé, Tina Kader, Gad Abikhzer, Stephan Probst
A 44-year-old woman was found to have new diffuse lung uptake on a follow-up whole-body I scan 1 year after being treated with surgery and radioactive iodine for papillary thyroid cancer. However, subsequent CT thorax and thyroglobulin levels were both unremarkable. Shortly after, she presented with respiratory symptoms, exhibiting end-expiratory wheezing on auscultation. Metacholine challenge test confirmed asthma. Symptoms improved under inhaled corticosteroids and beta-2 agonists. Resolution of lung uptake was confirmed on a second I imaging 6 months later...
April 2018: Clinical Nuclear Medicine
Anthony A Duplanty, Robert W Siggins, Timothy Allerton, Liz Simon, Patricia E Molina
Work from our group demonstrated that chronic binge alcohol (CBA)-induces mitochondrial gene dysregulation at end-stage disease of simian immunodeficiency virus (SIV) infection in antiretroviral therapy (ART) naïve rhesus macaques. Alterations in gene expression can disrupt mitochondrial homeostasis and in turn contribute to the risk of metabolic comorbidities characterized by loss of skeletal muscle (SKM) functional mass that are associated with CBA, human immunodeficiency virus (HIV) infection, and prolonged ART...
March 2018: Physiological Reports
Giulia Milano, Stefania Chiappini, Francesca Mattioli, Antonietta Martelli, Fabrizio Schifano
A recent years' increase in misusing levels of image- and performance- enhancing drugs (IPEDs) has been observed. Out of these drugs, beta-2 agonists have recently emerged for their potential of misuse, especially for slimming and bodybuilding purposes. To this perspective, clenbuterol ('the size zero pill') has been reported as being both popular and widely available from the illegal market. All clenbuterol and salbutamol misuse/abuse/dependence/withdrawal/overdose/off-label spontaneous reports (2006-2016) from the European Medicines Agency (EMA) EudraVigilance (EV) database were collected and analysed by age range, gender, concomitant therapies and source of information...
March 2, 2018: Basic & Clinical Pharmacology & Toxicology
Taedong Han, Byoung Moon Lee, Yoo Hoi Park, Dong Hoon Lee, Hyun Ho Choi, Taehoon Lee, Hakwon Kim
G protein-coupled receptor 119 (GPR119) is expressed in the pancreas and gastrointestinal tract, and its activation promotes insulin secretion in the beta cells of the pancreatic islets as well as the secretion of glucagon-like peptide-1 (GLP-1) in intestinal L cells, consequently improving glucose-stimulated insulin secretion. Due to this dual mechanism of action, the development of small-molecule GPR119 agonists has received significant interest for the treatment of type 2 diabetes. We newly synthesized 1,2,4-triazolone derivatives of GPR119 agonists, which demonstrated excellent outcomes in a cyclic adenosine monophosphate (cAMP) assay...
March 1, 2018: Biomolecules & Therapeutics
Cen Guo, Carl LaCerte, Jeffrey E Edwards, Kenneth R Brouwer, Kim L R Brouwer
Farnesoid X Receptor (FXR) is a nuclear receptor that regulates genes involved in bile acid homeostasis. FXR agonists, obeticholic acid (OCA) and chenodeoxycholic acid (CDCA), increase mRNA expression of efflux transporters in sandwich-cultured human hepatocytes (SCHH). This study evaluated the effects of OCA and CDCA treatment on the uptake, basolateral efflux, and biliary excretion of a model bile acid, taurocholate (TCA), in SCHH. Additionally, changes in the protein expression of TCA uptake and efflux transporters were investigated...
February 27, 2018: Journal of Pharmacology and Experimental Therapeutics
Raffaela Zaffini, Giovanni Gotte, Marta Menegazzi
Asthma is a chronic lung disease affecting people of all ages worldwide, and it frequently begins in childhood. Because of its chronic nature, it is characterized by pathological manifestations, including airway inflammation, remodeling, and goblet cell hyperplasia. Current therapies for asthma, including corticosteroids and beta-2 adrenergic agonists, are directed toward relieving the symptoms of the asthmatic response, with poor effectiveness against the underlying causes of the disease. Asthma initiation and progression depends on the T helper (Th) 2 type immune response carried out by a complex interplay of cytokines, such as interleukin (IL) 4, IL5, and IL13, and the signal transducer and activator of transcription 6...
2018: Drug Design, Development and Therapy
Andrew King, Mirjana Dimovska, Luke Bisoski
PURPOSE OF REVIEW: Acute drug-induced hypertension, sympathomimetic toxicity, and other hyperadrenergic states can be caused by both xenobiotic toxicity and withdrawal. This manuscript is a selective review of the recent literature regarding pharmacologic causes of hypertensive emergencies and other hyperadrenergic states. RECENT FINDINGS: We will discuss designer stimulants, alpha2 and baclofen agonist withdrawal, and the clinical entity known as posterior reversible encephalopathy syndrome (PRES)...
February 24, 2018: Current Hypertension Reports
Lei Lei, Yuanjie Mao
The common ultimate pathological feature for all cardiovascular diseases, congestive heart failure (CHF), is now considered as one of the main public health burdens that is associated with grave implications. Neurohormonal systems play a critical role in cardiovascular homeostasis, pathophysiology, and cardiovascular diseases. Hormone treatments such as the newly invented dual-acting drug valsartan/sacubitril are promising candidates for CHF, in addition to the conventional medications encompassing beta receptor blockers, angiotensin-converting enzyme inhibitors, angiotensin receptor blockers, and mineralocorticoid receptor antagonists...
January 1, 2018: Journal of International Medical Research
Gennaro Riccio, Salvatore Antonucci, Carmela Coppola, Chiara D'Avino, Giovanna Piscopo, Danilo Fiore, Carlo Maurea, Michele Russo, Domenica Rea, Claudio Arra, Gerolama Condorelli, Fabio Di Lisa, Carlo G Tocchetti, Claudia De Lorenzo, Nicola Maurea
The ErbB2 blocker trastuzumab improves survival in oncologic patients, but can cause cardiotoxicity. The late Na+ current inhibitor ranolazine has been shown to counter experimental HF, including doxorubicin cardiotoxicity (a condition characterized by derangements in redox balance), by lowering the levels of reactive oxygen species (ROS). Since ErbB2 can modulate ROS signaling, we tested whether trastuzumab cardiotoxicity could be blunted by ranolazine via redox-mediated mechanisms. Trastuzumab decreased fractional shortening and ejection fraction in mice, but ranolazine prevented heart dysfunction when co-administered with trastuzumab...
2018: Frontiers in Physiology
Grace McMacken, Dan Cox, Andreas Roos, Juliane Müller, Roger Whittaker, Hanns Lochmüller
Inherited defects of the neuromuscular junction (NMJ) comprise an increasingly diverse range of disorders, termed congenital myasthenic syndromes (CMS). Therapies acting on the sympathetic nervous system, including the selective β2 adrenergic agonist salbutamol and the α and β adrenergic agonist ephedrine, have become standard treatment for several types of CMS. However, the mechanism of the therapeutic effect of sympathomimetics in these disorders is not understood. Here, we examined the effect of salbutamol on NMJ development using zebrafish with deficiency of the key postsynaptic proteins Dok-7 and MuSK...
February 16, 2018: Human Molecular Genetics
T Heinosalo, M Gabriel, L Kallio, P Adhikari, K Huhtinen, T D Laajala, E Kaikkonen, A Mehmood, P Suvitie, H Kujari, T Aittokallio, A Perheentupa, M Poutanen
STUDY QUESTION: What is the role of SFRP2 in endometriosis? SUMMARY ANSWER: SFRP2 acts as a canonical WNT/CTNNB1 signaling agonist in endometriosis, regulating endometriosis lesion growth and indicating endometriosis lesion borders together with CTNNB1 (also known as beta catenin). WHAT IS KNOWN ALREADY: Endometriosis is a common, chronic disease that affects women of reproductive age, causing pain and infertility, and has significant economic impact on national health systems...
February 15, 2018: Human Reproduction
Sarah Petite
BACKGROUND: Chronic obstructive pulmonary disease (COPD) is the third-leading cause of death in the United States. Guideline recommendations for medication therapy include the use of inhaled medications for management of stable COPD. There are limited data available describing prescribing percentages of medications in patients with COPD. AIM: To determine the prescribing percentages of medications for COPD in a national, cross-sectional study. METHODS: This was a national, cross-sectional study using data from the National Ambulatory Medical Care Survey (NAMCS) in 2013...
February 15, 2018: Pulmonary Pharmacology & Therapeutics
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