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Metabolism , propranolol

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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
#1
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
#2
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...
July 6, 2017: Bone
https://www.readbyqxmd.com/read/28622605/flexible-nanofilms-coated-with-aligned-piezoelectric-microfibers-preserve-the-contractility-of-cardiomyocytes
#3
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
#4
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
#5
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
#6
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
#7
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
#8
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
https://www.readbyqxmd.com/read/28406442/liposomal-encapsulation-for-systemic-delivery-of-propranolol-via-transdermal-iontophoresis-improves-bone-microarchitecture-in-ovariectomized-rats
#9
Benjamin Teong, Shyh Ming Kuo, Wei-Hsin Tsai, Mei-Ling Ho, Chung-Hwan Chen, Han Hsiang Huang
The stimulatory effects of liposomal propranolol (PRP) on proliferation and differentiation of human osteoblastic cells suggested that the prepared liposomes-encapsulated PRP exerts anabolic effects on bone in vivo. Iontophoresis provides merits such as sustained release of drugs and circumvention of first pass metabolism. This study further investigated and evaluated the anti-osteoporotic effects of liposomal PRP in ovariectomized (OVX) rats via iontophoresis. Rats subjected to OVX were administered with pure or liposomal PRP via iontophoresis or subcutaneous injection twice a week for 12 weeks...
April 13, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28296053/vasoactive-effect-of-fibronectin-derived-epiviosamine-1-and-related-peptides-in-quiescent-and-stress-models
#10
Mary D Frame, Fubao Lin, Anthony M Dewar, Richard Af Clark
OBJECTIVE: Following thermal burn injury, plasma fibronectin degrades within the interstitium; one possible product is epiviosamine-1 (EVA-1, PSHISKYILRWRPK) found within the first type III repeat of plasma fibronectin (FNIII1 ). EVA-1 ameliorates thermal burn injury progression, and binds to and enhances platelet-derived growth factor-BB (PDGF-BB) in promoting cell metabolism, growth and survival; shorter related peptides lose these abilities. Here we study the effect of EVA-1 and shorter peptides for their vasoactivity under quiescent and stress conditions...
March 15, 2017: Microcirculation: the Official Journal of the Microcirculatory Society, Inc
https://www.readbyqxmd.com/read/28237652/impact-of-epinephrine-contained-in-local-anesthetic-solution-on-serum-lactate-level-during-orthognathic-surgery
#11
Hidetaka Kuroda, Gaku Kawamura, Manabu Soya, Takayuki Kitamura, Tatsuya Ichinohe, Yoshitsugu Yamada
PURPOSE: There have been many discussions of a relation between endogenous and exogenous epinephrine and hyperlactatemia. This study aimed to identify the impact of epinephrine contained in a local anesthetic solution on serum lactate levels in patients who underwent orthognathic surgery. MATERIALS AND METHODS: This study was a retrospective record review of cases of maxillary and mandibular osteotomy at the Tokyo University Hospital (Tokyo, Japan) from January 2006 through December 2014...
February 3, 2017: Journal of Oral and Maxillofacial Surgery
https://www.readbyqxmd.com/read/28236523/acute-but-not-chronic-exposure-to-arsenic-provokes-glucose-intolerance-in-rats-possible-roles-for-oxidative-stress-and-the-adrenergic-pathway
#12
Mohsen Rezaei, Mohammd Javad Khodayar, Enayatollah Seydi, Alboghobeish Soheila, Isa Kazemzadeh Parsi
OBJECTIVES: Health problems due to heavy metals have become a worldwide concern. Along with its carcinogenicity, arsenic exposure results in impairment of glucose metabolism and insulin secretion as well as altered gene expression and signal transduction. However, the exact mechanism behind the behaviour of arsenic on glucose homeostasis and insulin secretion has not yet been fully understood. METHODS: Fasting blood sugar and glucose tolerance tests were evaluated...
February 21, 2017: Canadian Journal of Diabetes
https://www.readbyqxmd.com/read/28126832/effect-of-%C3%AE-agonist-on-the-dexamethasone-induced-expression-of-aromatase-by-the-human-monocyte-cells
#13
Masatada Watanabe, Shuji Ohno, Hiroshi Wachi
Emerging evidence suggests that sex steroids are important for human skin health. In particular, estrogen improves skin thickness, elasticity and moisture of older women. The major source of circulating estrogen is the ovary; however, local estrogen synthesis and secretion have important roles in, for example, bone metabolism and breast cancer development. We hypothesized that infiltrated peripheral monocytes are one of the sources of estrogen in skin tissues. We also hypothesized that, during atopic dermatitis under stress, a decline in the hypothalamus-pituitary-adrenal axis (HPA) and facilitation of the (hypothalamus)-sympathetic-adrenomedullary system (SAM) attenuates estrogen secretion from monocytes...
February 2017: Endocrine Connections
https://www.readbyqxmd.com/read/28045944/pharmaceutical-metabolism-in-fish-using-a-3-d-hepatic-in-vitro-model-to-assess-clearance
#14
Matthew G Baron, Kate S Mintram, Stewart F Owen, Malcolm J Hetheridge, A John Moody, Wendy M Purcell, Simon K Jackson, Awadhesh N Jha
At high internal doses, pharmaceuticals have the potential for inducing biological/pharmacological effects in fish. One particular concern for the environment is their potential to bioaccumulate and reach pharmacological levels; the study of these implications for environmental risk assessment has therefore gained increasing attention. To avoid unnecessary testing on animals, in vitro methods for assessment of xenobiotic metabolism could aid in the ecotoxicological evaluation. Here we report the use of a 3-D in vitro liver organoid culture system (spheroids) derived from rainbow trout to measure the metabolism of seven pharmaceuticals using a substrate depletion assay...
2017: PloS One
https://www.readbyqxmd.com/read/28002075/what-factors-influence-protein-synthesis-and-degradation-in-critical-illness
#15
Filippo G Di Girolamo, Roberta Situlin, Gianni Biolo
PURPOSE OF REVIEW: The optimal approach to improve protein metabolism in critical illness is not yet fully defined. Here, we have summarized recent literature dealing with the main catabolic and anabolic factors influencing protein kinetics in acute hypercatabolic patients. RECENT FINDINGS: Protein/amino acid intake levels should be adapted to type and severity of illness, keeping in mind that energy overfeeding is associated with poor outcome. A number of anticatabolic nutraceuticals and drugs have been tested in acute patients...
March 2017: Current Opinion in Clinical Nutrition and Metabolic Care
https://www.readbyqxmd.com/read/27902848/topiramate-in-migraine-prevention-a-2016-perspective
#16
REVIEW
Stephen D Silberstein
BACKGROUND: In evidence-based guidelines published in 2000, topiramate was a third-tier migraine preventive with no scientific evidence of efficacy; recommendation for its use reflected consensus opinion and clinical experience. Its neurostabilizing activity, coupled with its favorable weight profile, made topiramate an attractive alternative to other migraine preventives that caused weight gain. When guidelines for migraine prevention in episodic migraine were published in 2012, topiramate was included as a first-line option based on double-blind, randomized controlled trials involving nearly 3000 patients...
January 2017: Headache
https://www.readbyqxmd.com/read/27790765/acupuncture-does-not-ameliorate-metabolic-disturbances-in-the-p450-aromatase-inhibitor-induced-rat-model-of-polycystic-ovary-syndrome
#17
Manuel Maliqueo, Anna Benrick, Rodrigo Rodrigues Marcondes, Julia Johansson, Miao Sun, Elisabet Stener-Victorin
What is the central question of this study? The effectiveness of low-frequency electroacupuncture in the treatment of metabolic disorders associated with polycystic ovary syndrome (PCOS), an endocrine-metabolic disorder characterized by an imbalance in sex steroid production, is controversial. What is the main finding and its importance? In a rat model of PCOS induced by the inhibition of P450 aromatase, low-frequency electroacupuncture increased low-density lipoprotein-cholesterol but did not improve the insulin resistance or the adipose tissue dysfunction, suggesting that a balance of sex steroids is needed to restore the metabolic function in this rat model of PCOS...
January 1, 2017: Experimental Physiology
https://www.readbyqxmd.com/read/27760784/quantitative-assessment-of-population-variability-in-hepatic-drug-metabolism-using-a-perfused-three-dimensional-human-liver-microphysiological-system
#18
N Tsamandouras, T Kostrzewski, C L Stokes, L G Griffith, D J Hughes, M Cirit
In this work, we first describe the population variability in hepatic drug metabolism using cryopreserved hepatocytes from five different donors cultured in a perfused three-dimensional human liver microphysiological system, and then show how the resulting data can be integrated with a modeling and simulation framework to accomplish in vitro-in vivo translation. For each donor, metabolic depletion profiles of six compounds (phenacetin, diclofenac, lidocaine, ibuprofen, propranolol, and prednisolone) were measured, along with metabolite formation, mRNA levels of 90 metabolism-related genes, and markers of functional viability [lactate dehydrogenase (LDH) release, albumin, and urea production]...
January 2017: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/27650667/the-effects-of-feeding-on-cardiac-control-of-the-broad-nosed-caiman-caiman-latirostris-the-role-of-the-autonomic-nervous-system-and-nanc-factors
#19
Victor Hugo DA Silva Braga, Vinicius Araújo Armelin, Mariana Teodoro Teixeira, Augusto Shinya Abe, Francisco Tadeu Rantin, Luiz Henrique Florindo
The metabolic increment that occurs after feeding demands cardiovascular adjustments to be maintained, as increased heart rate (fH ) and cardiac output. In mammals, postprandial tachycardia seems to be triggered by an increase in adrenergic activity and by nonadrenergic noncholinergic (NANC) factors, while in ectothermic vertebrates, this adjustment seems to be linked to a withdrawal of vagal drive as well as to NANC factors. Because the factors behind postprandial tachycardia have not yet been investigated in crocodilians, the present study sought to evaluate the postprandial tachycardia mediators in the broad-nosed caiman...
September 21, 2016: Journal of Experimental Zoology. Part A, Ecological Genetics and Physiology
https://www.readbyqxmd.com/read/27571995/metabolomic-responses-to-sublethal-contaminant-exposure-in-neonate-and-adult-daphnia-magna
#20
Nicole D Wagner, André J Simpson, Myrna J Simpson
The use of consumer products and pharmaceuticals that act as contaminants entering waterways through runoff and wastewater effluents alters aquatic ecosystem health. Traditional toxicological endpoints may underestimate the toxicity of contaminants, as lethal concentrations are often orders of magnitude higher than those found within freshwater ecosystems. While newer techniques examine the metabolic responses of sublethal contaminant exposure, there has been no direct comparison with ontogeny in Daphnia. It was hypothesized that Daphnia magna would have distinct metabolic changes after 3 different sublethal contaminant exposures, because of differences in the toxic mode of action and ontogeny...
April 2017: Environmental Toxicology and Chemistry
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