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Metabolism , propranolol

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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
#1
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
#2
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.
January 8, 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
#3
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
#4
Francesca Leanne Wood, James 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 measurement of intrinsic hepatic clearance mediated by active uptake transport and metabolism, lack of prediction reliability appears to reflect a lack of methodological validation, especially for highly cleared drugs, as we have previously shown...
December 12, 2017: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/29214053/severe-carvedilol-toxicity-without-overdose-caution-in-cirrhosis
#5
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
#6
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...
November 16, 2017: Life Sciences
https://www.readbyqxmd.com/read/29110304/beta-blockers-for-preventing-aortic-dissection-in-marfan-syndrome
#7
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
#8
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
#9
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)...
September 26, 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
#10
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
#11
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 are however not 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) mice and LOX/LOX 1) 3h after a single exercise bout with or without prior injection of propranolol or 3h after a single injection of clenbuterol and 2) after 5 weeks of wheel running exercise training with or without propranolol treatment or after 5 weeks of clenbuterol treatment...
September 5, 2017: American Journal of Physiology. Endocrinology and Metabolism
https://www.readbyqxmd.com/read/28844874/cannabinoid-cb1-receptor-inverse-agonist-mj08-stimulates-glucose-production-via-hepatic-sympathetic-innervation-in-rats
#12
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
#13
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
https://www.readbyqxmd.com/read/28689816/a-novel-role-for-dopamine-signaling-in-the-pathogenesis-of-bone-loss-from-the-atypical-antipsychotic-drug-risperidone-in-female-mice
#14
Katherine J Motyl, Megan Beauchemin, Deborah Barlow, Phuong T Le, Kenichi Nagano, Annika Treyball, Anisha Contractor, Roland Baron, Clifford J Rosen, Karen L Houseknecht
Atypical antipsychotic (AA) drugs, including risperidone (RIS), are used to treat schizophrenia, bipolar disorder, and autism, and are prescribed off-label for other mental health issues. AA drugs are associated with severe metabolic side effects of obesity and type 2 diabetes. Cross-sectional and longitudinal data also show that risperidone causes bone loss and increases fracture risk in both men and women. There are several potential mechanisms of bone loss from RIS. One is hypogonadism due to hyperprolactinemia from dopamine receptor antagonism...
October 2017: Bone
https://www.readbyqxmd.com/read/28622605/flexible-nanofilms-coated-with-aligned-piezoelectric-microfibers-preserve-the-contractility-of-cardiomyocytes
#15
P José Gouveia, S Rosa, L Ricotti, B Abecasis, H V Almeida, L Monteiro, J Nunes, F Sofia Carvalho, M Serra, S Luchkin, A Leonidovitch Kholkin, P Marques Alves, P Jorge Oliveira, R Carvalho, A Menciassi, R Pires das Neves, L Silva Ferreira
The use of engineered cardiac tissue for high-throughput drug screening/toxicology assessment remains largely unexplored. Here we propose a scaffold that mimics aspects of cardiac extracellular matrix while preserving the contractility of cardiomyocytes. The scaffold is based on a poly(caprolactone) (PCL) nanofilm with magnetic properties (MNF, standing for magnetic nanofilm) coated with a layer of piezoelectric (PIEZO) microfibers of poly(vinylidene fluoride-trifluoroethylene) (MNF+PIEZO). The nanofilm creates a flexible support for cell contraction and the aligned PIEZO microfibers deposited on top of the nanofilm creates conditions for cell alignment and electrical stimulation of the seeded cells...
September 2017: Biomaterials
https://www.readbyqxmd.com/read/28580281/glucagon-like-peptide-2-promotes-gallbladder-refilling-via-a-tgr5-independent-glp-2r-dependent-pathway
#16
Bernardo Yusta, Dianne Matthews, Grace B Flock, John R Ussher, Brigitte Lavoie, Gary M Mawe, Daniel J Drucker
OBJECTIVE: Glucagon-like peptides (GLPs) are secreted from enteroendocrine cells in response to nutrients and bile acids and control metabolism via actions on structurally-related yet distinct G protein coupled receptors. GLP-1 regulates gut motility, appetite, islet function, and glucose homeostasis, whereas GLP-2 enhances intestinal nutrient absorption. GLP-1R agonists are used to treat diabetes and obesity, and a GLP-2R agonist is approved to treat short bowel syndrome. Unexpectedly, reports of gallbladder disease have been associated with the use of both GLP-1R and GLP-2R agonists and after bariatric surgery, although the mechanisms remain unknown...
June 2017: Molecular Metabolism
https://www.readbyqxmd.com/read/28554023/uptake-biotransformation-and-elimination-of-selected-pharmaceuticals-in-a-freshwater-invertebrate-measured-using-liquid-chromatography-tandem-mass-spectrometry
#17
Thomas H Miller, Nicolas R Bury, Stewart F Owen, Leon P Barron
Methods were developed to assess uptake and elimination kinetics in Gammarus pulex of nine pharmaceuticals (sulfamethazine, carbamazepine, diazepam, temazepam, trimethoprim, warfarin, metoprolol, nifedipine and propranolol) using targeted LC-MS/MS to determine bioconcentration factors (BCFs) using a 96 h toxicokinetic exposure and depuration period. The derived BCFs for these pharmaceuticals did not trigger any regulatory thresholds and ranged from 0 to 73 L kg(-1) (sulfamethazine showed no bioconcentration)...
September 2017: Chemosphere
https://www.readbyqxmd.com/read/28548953/from-rapalogs-to-anti-aging-formula
#18
Mikhail V Blagosklonny
Inhibitors of mTOR, including clinically available rapalogs such as rapamycin (Sirolimus) and Everolimus, are gerosuppressants, which suppress cellular senescence. Rapamycin slows aging and extends life span in a variety of species from worm to mammals. Rapalogs can prevent age-related diseases, including cancer, atherosclerosis, obesity, neurodegeneration and retinopathy and potentially rejuvenate stem cells, immunity and metabolism. Here, I further suggest how rapamycin can be combined with metformin, inhibitors of angiotensin II signaling (Losartan, Lisinopril), statins (simvastatin, atorvastatin), propranolol, aspirin and a PDE5 inhibitor...
May 30, 2017: Oncotarget
https://www.readbyqxmd.com/read/28502673/glucosamine-modulates-propranolol-pharmacokinetics-via-intestinal-permeability-in-rats
#19
Hanadi A Al Shaker, Nidal A Qinna, Mujtaba Badr, Mahmoud M H Al Omari, Nasir Idkaidek, Khalid Z Matalka, Adnan A Badwan
Propranolol (PROP) undergoes extensive first-pass metabolism by the liver resulting in a relatively low bioavailability (13-23%); thus, multiple oral doses are required to achieve therapeutic effect. Since some studies have reported that glucosamine (GlcN) can increase the bioavailability of some drugs, therefore, it is aimed to study whether GlcN can change the pharmacokinetic parameters of PROP, thus modulating its bioavailability. When PROP was orally co-administered with GlcN (200mg/kg) to rats, PROP area under curve (AUC) and maximum concentration (Cmax) were significantly decreased by 43% (p<0...
May 11, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28454738/rat-brain-cyp2d-enzymatic-metabolism-alters-acute-and-chronic-haloperidol-side-effects-by-different-mechanisms
#20
Sharon Miksys, Fariba Baghai Wadji, Edgor Cole Tolledo, Gary Remington, Jose N Nobrega, Rachel F Tyndale
Risk for side-effects after acute (e.g. parkinsonism) or chronic (e.g. tardive dyskinesia) treatment with antipsychotics, including haloperidol, varies substantially among people. CYP2D can metabolize many antipsychotics and variable brain CYP2D metabolism can influence local drug and metabolite levels sufficiently to alter behavioral responses. Here we investigated a role for brain CYP2D in acutely and chronically administered haloperidol levels and side-effects in a rat model. Rat brain, but not liver, CYP2D activity was irreversibly inhibited with intracerebral propranolol and/or induced by seven days of subcutaneous nicotine pre-treatment...
April 26, 2017: Progress in Neuro-psychopharmacology & Biological Psychiatry
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