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Metabolism , propranolol

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https://www.readbyqxmd.com/read/29774054/beta-adrenoceptor-blockade-ameliorates-impaired-glucose-tolerance-and-alterations-of-the-cerebral-ceramide-metabolism-in-an-experimental-model-of-ischemic-stroke
#1
Sebastian Luger, Annette Schwebler, Rajkumar Vutukuri, Nerea Ferreiros Bouzas, Sandra Labocha, Yannick Schreiber, Robert Brunkhorst, Helmuth Steinmetz, Josef Pfeilschifter, Waltraud Pfeilschifter
Background: Sphingolipids are versatile signaling molecules derived from membrane lipids of eukaryotic cells. Ceramides regulate cellular processes such as proliferation, differentiation and apoptosis and are involved in cellular stress responses. Experimental evidence suggests a pivotal role of sphingolipids in the pathogenesis of cardiovascular diseases, including ischemic stroke. A neuroprotective effect has been shown for beta-adrenergic antagonists in rodent stroke models and supported by observational clinical data...
2018: Therapeutic Advances in Neurological Disorders
https://www.readbyqxmd.com/read/29728578/propranolol-sensitizes-prostate-cancer-cells-to-glucose-metabolism-inhibition-and-prevents-cancer-progression
#2
Laura Brohée, Olivier Peulen, Betty Nusgens, Vincent Castronovo, Marc Thiry, Alain C Colige, Christophe F Deroanne
Propranolol, a widely used non-selective beta-adrenergic receptor blocker, was recently shown to display anticancer properties. Its potential to synergize with certain drugs has been also outlined. However, it is necessary to take into account all the properties of propranolol to select a drug that could be efficiently combined with. Propranolol was reported to block the late phase of autophagy. Hence, we hypothesized that in condition enhancing autophagy flux, cancer cells should be especially sensitive to propranolol...
May 4, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29554753/effects-of-dissolved-organic-matter-and-nitrification-on-biodegradation-of-pharmaceuticals-in-aerobic-enrichment-cultures
#3
Yujie He, Alette A M Langenhoff, Rob N J Comans, Nora B Sutton, Huub H M Rijnaarts
Natural dissolved organic matter (DOM) and nitrification can play an important role in biodegradation of pharmaceutically active compounds (PhACs) in aerobic zones of constructed wetlands (CWs). This study used an enrichment culture originating from CW sediment to study the effect of DOM and nitrification on aerobic biodegradation of seven PhACs. The enriched culture degraded caffeine (CAF), metoprolol (MET), naproxen (NAP), and ibuprofen (IBP) with a consistent biodegradability order of CAF>MET>NAP>IBP...
March 2, 2018: Science of the Total Environment
https://www.readbyqxmd.com/read/29554612/environmental-concentrations-of-pharmaceuticals-directly-affect-phytoplankton-and-effects-propagate-through-trophic-interactions
#4
Malgorzata Grzesiuk, Elly Spijkerman, Sabrina C Lachmann, Alexander Wacker
Pharmaceuticals are found in freshwater ecosystems where even low concentrations in the range of ng L-1 may affect aquatic organisms. In the current study, we investigated the effects of chronic exposure to three pharmaceuticals on two microalgae, a potential modulation of the effects by additional inorganic phosphorus (Pi ) limitation, and a potential propagation of the pharmaceuticals' effect across a trophic interaction. The latter considers that pharmaceuticals are bioaccumulated by algae, potentially metabolized into more (or less) toxic derivates and consequently consumed by zooplankton...
March 16, 2018: Ecotoxicology and Environmental Safety
https://www.readbyqxmd.com/read/29546518/assessment-of-biochemical-alterations-in-the-neotropical-fish-species-phalloceros-harpagos-after-acute-and-chronic-exposure-to-the-drugs-paracetamol-and-propranolol
#5
Beatriz V R Pereira, Gregorio Nolazco Matus, Monica Jones Costa, André Cordeiro Alves Dos Santos, Elaine C M Silva-Zacarin, Janaina Braga do Carmo, Bruno Nunes
Over time, many pollutants of anthropogenic origin have caused the contamination of aquatic ecosystems. Among several characteristics, these compounds can reach the trophic chain, causing deleterious interactions with the biota. Pharmaceutical substances can be included in this scenario as emerging contaminants that reach the aquatic environment because of direct human and veterinary usage, and release by industrial effluents, as well as through domestic dumping of surplus drugs. The effects of these compounds on exposed organisms have been studied since the 1990s, but ecotoxicological data for such chemicals are still scarce especially concerning aquatic organisms from tropical regions...
March 15, 2018: Environmental Science and Pollution Research International
https://www.readbyqxmd.com/read/29504260/dietary-tryptophan-restriction-dose-dependently-modulates-energy-balance-gut-hormones-and-microbiota-in-obesity-prone-rats
#6
Rizaldy C Zapata, Arashdeep Singh, Nadia M Ajdari, Prasanth K Chelikani
OBJECTIVE: To determine the effects of graded dietary restriction of tryptophan on food intake, energy expenditure, body composition, gut hormones, and select fecal bacterial populations in obesity-prone rats. METHODS: Obesity-prone rats were randomized to isocaloric diets with varying degrees of tryptophan restriction: control (100% requirements), 70% tryptophan (70TRP), 40% tryptophan (40TRP), or 10% tryptophan (10TRP) for 21 days. The sympathetic system was challenged with a subcutaneous injection of propranolol on days 15 to 17...
April 2018: Obesity
https://www.readbyqxmd.com/read/29437806/rhabdomyolysis-in-stuve-wiedemann-syndrome
#7
Pemantah Sandheeah Ramdeny, Colin Powell, Mallinath Chakraborty, Louise Hartley
A 6-month-old male infant with Stuve-Wiedemann syndrome (SWS) presented with an acute respiratory arrest secondary to a rhinovirus respiratory infection from which he was rapidly resuscitated. He developed an acute kidney injury requiring supportive treatment and on day 3 of his illness was noted to have developed severe rhabdomyolysis (creatine kinase level 132 040 U/L (normal <320 U/L)). He was born from consanguineous parents with homozygous mutations in the leukaemia inhibitory factor receptor. He had skeletal dysplasia with metabolic bone disease and episodes of hyperthermia with lactic acidosis...
February 8, 2018: BMJ Case Reports
https://www.readbyqxmd.com/read/29313295/radiation-preparation-of-l-arginine-acrylic-acid-hydrogel-matrix-patch-for-transdermal-delivery-of-propranolol-hcl-in-hypertensive-rats
#8
Rasha R Radwan, Heba A Mohamed, H E Ali, Ghada A Mahmoud
In the present study, L-arginine/acrylic acid (Arg/AAc) batch hydrogel was successfully prepared by gamma irradiation for transdermal delivery of propranolol HCl in hypertensive rats. The resulted system has been characterized by FTIR to confirm the hydrogel formation. The swelling behavior of the prepared hydrogels was investigated as a function of time and pH. The kinetics of swelling has been investigated. In vivo pharmacokinetics evaluation, skin irritation test, and histopathological studies were investigated...
January 8, 2018: Drug Delivery and Translational Research
https://www.readbyqxmd.com/read/29306335/recurrent-hypoglycaemia-in-a-toddler-on-%C3%AE-blocker-therapy
#9
Véronique Pépin, Nancy Gagné, Diane Rottembourg
Hypoglycaemia is a well-known side effect of Propranolol. We described the case of a child presenting severe and recurrent Propranolol-induced hypoglycaemia. Those episodes were not related to prolonged fasting and were associated with only mild ketosis. Thus, therapy with β blockers may not only aggravate classical ketotic hypoglycaemia but also interfere with glucose metabolism.
March 2018: Cardiology in the Young
https://www.readbyqxmd.com/read/29275472/the-impact-of-housing-temperature-induced-chronic-stress-on-preclinical-mouse-tumor-models-and-therapeutic-responses-an-important-role-for-the-nervous-system
#10
Bonnie L Hylander, Jason W-L Eng, Elizabeth A Repasky
In the last 10-15 years, there has been a recognition that the catecholamines (norepinephrine, NE, and epinephrine, Epi) released by the sympathetic nervous system under stressful conditions promote tumor growth through a variety of mechanisms. Tumors recruit autonomic nerves during their development and NE is then released locally in the tumor microenvironment (TME). Acting through adrenergic receptors present on a variety of cells in the TME, NE and Epi induce proliferation, resistance to apoptosis, epithelial to mesenchymal transition, metastasis of tumor cells, angiogenesis, and inflammation in the TME...
2017: Advances in Experimental Medicine and Biology
https://www.readbyqxmd.com/read/29233818/importance-of-the-unstirred-water-layer-and-hepatocyte-membrane-integrity-in-vitro-for-quantification-of-intrinsic-metabolic-clearance
#11
Francesca L Wood, J Brian Houston, David Hallifax
Prediction of clearance-a vital component of drug discovery-remains in need of improvement and, in particular, requires more incisive assessment of mechanistic methodology in vitro, according to a number of recent reports. Although isolated hepatocytes have become an irreplaceable standard system for the measurement of intrinsic hepatic clearance mediated by active uptake transport and metabolism, the lack of prediction reliability appears to reflect a lack of methodological validation, especially for highly cleared drugs, as we have previously shown...
March 2018: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/29214053/severe-carvedilol-toxicity-without-overdose-caution-in-cirrhosis
#12
Satish Maharaj, Karan Seegobin, Julio Perez-Downes, Belinda Bajric, Simone Chang, Pramod Reddy
Background: Carvedilol is used in the management of hypertension, ischemic heart disease, heart failure and most recently, portal hypertension. It has been associated with improved outcomes regarding variceal bleeding, hepatic decompensation and death when compared to propranolol and endoscopic band ligation. The main cause of portal hypertension is cirrhosis and therefore carvedilol is increasingly used in these patients. Due to its extensive hepatic metabolism, carvedilol is contraindicated in severe hepatic impairment...
2017: Clinical Hypertension
https://www.readbyqxmd.com/read/29155297/divergent-profile-between-hypothalamic-and-plasmatic-aminopeptidase-activities-in-wky-and-shr-influence-of-beta-adrenergic-blockade
#13
REVIEW
Isabel Prieto, Ana B Segarra, Marc de Gasparo, Magdalena Martínez-Cañamero, Manuel Ramírez-Sánchez
AIMS: Wistar-Kyoto (WKY) and spontaneously hypertensive rats (SHR) differ in their renin-angiotensin system function and sympathetic tone. The metabolism of angiotensins and vasopressin depends on the action of certain aminopeptidases whose activity may be influenced by the autonomic nervous system. Their regulation may differ between WKY and SHR in hypothalamus and plasma according to the sympathetic tone. We analyzed aminopeptidases responsible for the hydrolysis of certain angiotensins, vasopressin, cholecystokinin or enkephalins in hypothalamus and plasma of WKY and SHR in untreated controls rats and under beta-adrenoceptor blockade...
January 1, 2018: Life Sciences
https://www.readbyqxmd.com/read/29110304/beta-blockers-for-preventing-aortic-dissection-in-marfan-syndrome
#14
REVIEW
Hyun-Kyoung Koo, Kendra Ak Lawrence, Vijaya M Musini
BACKGROUND: Marfan syndrome is a hereditary disorder affecting the connective tissue and is caused by a mutation of the fibrillin-1 (FBN1) gene. It affects multiple systems of the body, most notably the cardiovascular, ocular, skeletal, dural and pulmonary systems. Aortic root dilatation is the most frequent cardiovascular manifestation and its complications, including aortic regurgitation, dissection and rupture are the main cause of morbidity and mortality. OBJECTIVES: To assess the long-term efficacy and safety of beta-blocker therapy as compared to placebo, no treatment or surveillance only in people with Marfan syndrome...
November 7, 2017: Cochrane Database of Systematic Reviews
https://www.readbyqxmd.com/read/29107282/the-autonomic-nervous-system-and-cardiac-glp-1-receptors-control-heart-rate-in-mice
#15
Laurie L Baggio, John R Ussher, Brent A McLean, Xiemin Cao, M Golam Kabir, Erin E Mulvihill, Alexandra S Mighiu, Hangjun Zhang, Andreas Ludwig, Randy J Seeley, Scott P Heximer, Daniel J Drucker
OBJECTIVES: Glucagon-like peptide-1 (GLP-1) is secreted from enteroendocrine cells and exerts a broad number of metabolic actions through activation of a single GLP-1 receptor (GLP-1R). The cardiovascular actions of GLP-1 have garnered increasing attention as GLP-1R agonists are used to treat human subjects with diabetes and obesity that may be at increased risk for development of heart disease. Here we studied mechanisms linking GLP-1R activation to control of heart rate (HR) in mice...
November 2017: Molecular Metabolism
https://www.readbyqxmd.com/read/28948673/piperine-decreases-binding-of-drugs-to-human-plasma-and-increases-uptake-by-brain-microvascular-endothelial-cells
#16
Raghvendra K Dubey, Brigitte Leeners, Bruno Imthurn, Gabriele Susanne Merki-Feld, Marinella Rosselli
We previously reported that piperine, an active alkaloidal principal of black and long peppers, enhances drug bioavailability by inhibiting drug metabolism. Another mechanism influencing drug availability/uptake is its free fraction. Since piperine is highly lipophilic, we hypothesize that it could also interact with drugs through binding displacement and influence their bioavailability. Accordingly, using equilibrium dialysis, we investigated whether piperine alters the binding of model drug ligands, that is flunitrazepam, diazepam, warfarin, salicylic acid, propranolol, lidocaine, and disopyramide to human plasma (n = 4)...
December 2017: Phytotherapy Research: PTR
https://www.readbyqxmd.com/read/28917751/structural-characterization-of-electrochemically-and-in-vivo-generated-potential-metabolites-of-selected-cardiovascular-drugs-by-ec-uhplc-esi-ms-using-an-experimental-design-approach
#17
Małgorzata Szultka-Młyńska, Sylwia Bajkacz, Irena Baranowska, Bogusław Buszewski
In the last few years, a number of studies were conducted which aimed at understanding the mechanisms of cardiovascular drug, metabolism, and there is still the need to determine the metabolites of cardiac drugs for the purpose of metabolism control. In this study, we employ a direct combination of electrochemical oxidation and mass spectrometric (EC-MS) identification for monitoring the oxidation pathway of ten cardiovascular drugs (metoprolol, propranolol, propafenone, mexiletine, oxprenolol, pirbuterol, pindolol, cicloprolol, acebutolol and atenolol)...
January 1, 2018: Talanta
https://www.readbyqxmd.com/read/28874356/impact-of-%C3%AE-adrenergic-signaling-in-pgc-1%C3%AE-mediated-adaptations-in-mouse-skeletal-muscle
#18
Nina Brandt, Lene Nielsen, Bjørg Thiellesen Buch, Anders Gudiksen, Stine Ringholm, Ylva Hellsten, Jens Bangsbo, Henriette Pilegaard
PGC-1α has been suggested to regulate exercise training-induced metabolic adaptations and autophagy in skeletal muscle. The factors regulating PGC-1α, however, have not been fully resolved. The aim was to investigate the impact of β-adrenergic signaling in PGC-1α-mediated metabolic adaptations in skeletal muscle with exercise training. Muscle was obtained from muscle-specific PGC-1α knockout (MKO) and lox/lox mice 1) 3 h after a single exercise bout with or without prior injection of propranolol or 3 h after a single injection of clenbuterol and 2) after 5 wk of wheel running exercise training with or without propranolol treatment or after 5 wk of clenbuterol treatment...
January 1, 2018: American Journal of Physiology. Endocrinology and Metabolism
https://www.readbyqxmd.com/read/28844874/cannabinoid-cb-1-receptor-inverse-agonist-mj08-stimulates-glucose-production-via-hepatic-sympathetic-innervation-in-rats
#19
Wei Chen, Hongying Liu, Hua Guan, Nina Xue, Lili Wang
As a key insulin target tissue for maintaining systemic glucose homeostasis, the liver plays important roles in improving obesity-associated insulin intolerance via selective cannabinoid CB1 receptor antagonism/inverse agonism. However, it is unclear whether this receptor inverse agonism affects hepatic glucose metabolism. MJ08 is a novel cannabinoid CB1 receptor antagonist/inverse agonist that has superior inverse agonism over the well-known antagonist/inverse agonist, SR141716 (rimonabant). MJ08 remarkably elevates fasting blood glucose independent of inhibition of insulin release in mice...
November 5, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28709412/study-protocol-safety-and-efficacy-of-propranolol-0-2-eye-drops-in-newborns-with-a-precocious-stage-of-retinopathy-of-prematurity-drop-rop-0-2-a-multicenter-open-label-single-arm-phase-ii-trial
#20
MULTICENTER STUDY
Luca Filippi, Giacomo Cavallaro, Elettra Berti, Letizia Padrini, Gabriella Araimo, Giulia Regiroli, Valentina Bozzetti, Chiara De Angelis, Paolo Tagliabue, Barbara Tomasini, Giuseppe Buonocore, Massimo Agosti, Angela Bossi, Gaetano Chirico, Salvatore Aversa, Roberta Pasqualetti, Pina Fortunato, Silvia Osnaghi, Barbara Cavallotti, Maurizio Vanni, Giulia Borsari, Simone Donati, Giuseppe Nascimbeni, Giancarlo la Marca, Giulia Forni, Silvano Milani, Ivan Cortinovis, Paola Bagnoli, Massimo Dal Monte, Anna Maria Calvani, Alessandra Pugi, Eduardo Villamor, Gianpaolo Donzelli, Fabio Mosca
BACKGROUND: Retinopathy of prematurity (ROP) still represents one of the leading causes of visual impairment in childhood. Systemic propranolol has proven to be effective in reducing ROP progression in preterm newborns, although safety was not sufficiently guaranteed. On the contrary, topical treatment with propranolol eye micro-drops at a concentration of 0.1% had an optimal safety profile in preterm newborns with ROP, but was not sufficiently effective in reducing the disease progression if administered at an advanced stage (during stage 2)...
July 14, 2017: BMC Pediatrics
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