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Carvedilol

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https://www.readbyqxmd.com/read/28531555/microbial-detoxification-of-carvedilol-a-%C3%AE-adrenergic-antagonist-by-the-filamentous-fungus-cunninghamella-echinulata
#1
Katarzyna Zawadzka, Przemysław Bernat, Aleksandra Felczak, Katarzyna Lisowska
Beta adrenergic antagonists like carvedilol are typical environmental pollutants detected in wastewater and surface water. Human metabolism of carvedilol is well investigated, while its environmental fates are still unknown. In recent years, there have been appearing reports on high toxicity of β-blockers toward aquatic organisms. In this paper the ability of the filamentous fungus C. echinulata to eliminate the β-blocker has been described for the first time. An 83% loss of carvedilol was observed after 120 h incubation of the tested fungus with the compound, where hydroxylated carvedilol metabolites were identified as the major biotransformation products...
May 16, 2017: Chemosphere
https://www.readbyqxmd.com/read/28527109/erratum-to-clinical-pharmacokinetics-of-sacubitril-valsartan-lcz696-a-novel-angiotensin-receptor-neprilysin-inhibitor
#2
Surya Ayalasomayajula, Thomas Langenickel, Parasar Pal, Sreedevi Boggarapu, Gangadhar Sunkara
Sacubitril/valsartan (LCZ696) is indicated for the treatment of heart failure with reduced ejection fraction. Absorption of sacubitril/valsartan and conversion of sacubitril (prodrug) to sacubitrilat (neprilysin inhibitor) was rapid with maximum plasma concentrations of sacubitril, sacubitrilat, and valsartan (angiotensin receptor blocker) reaching within 0.5, 1.5-2.0, and 2.0-3.0 h, respectively. With a twofold increase in dose, an increase in the area under the plasma concentration-time curve was proportional for sacubitril, ~1...
May 19, 2017: Clinical Pharmacokinetics
https://www.readbyqxmd.com/read/28523858/clinical-signs-diagnostics-and-successful-treatment-of-a-myocarditis-in-an-adult-chimpanzee-pan-troglodytes
#3
Martine van Zijll Langhout, Marno Wolters, Katalin M Horvath, Harold Thiesbrummel, Paul Smits, Hester van Bolhuis, Victor van der Hulst, Robert Riezebos
A chimpanzee (Pan troglodytes) was presented with lethargic behaviour. Echocardiography and abnormal cardiac and inflammatory biomarkers revealed a myocarditis. The animal fully recovered after prolonged treatment with losartan and carvedilol. This is the first report of the diagnosis and successful treatment of myocarditis in this species.
May 19, 2017: Journal of Medical Primatology
https://www.readbyqxmd.com/read/28522373/population-pharmacokinetics-of-carvedilol-enantiomers-and-their-metabolites-in-type-2-diabetes-and-healthy-subjects
#4
Glauco H B Nardotto, Vera L Lanchote, Eduardo B Coelho, Oscar Della Pasqua
Carvedilol, a drug available as a racemic mixture, is eliminated as hydroxyphenylcarvedilol (OHC) by CYP2D6 and O-desmethylcarvedilol (DMC) by CYP2C9 followed by conjugation to glucuronides. In contrast to other β-adrenergic receptor antagonists, carvedilol does not induce insulin resistance or worsen glycaemic control in the diabetic hypertensive patients. This study aims to investigate the implications of type 2 diabetes (T2DM) on the pharmacokinetics of carvedilol enantiomers using an integrated population pharmacokinetic modelling approach...
May 15, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28520538/treatment-strategies-for-paradoxical-hypertension-following-surgical-correction-of-coarctation-of-the-aorta-in-children
#5
Peter P Roeleveld, Eline G Zwijsen
BACKGROUND: Paradoxical hypertension after repair of coarctation of the aorta is a well-known phenomenon. The pathogenesis involves the activation of the sympathetic nervous system (first phase) and renin-angiotensin system (second phase). Only a limited number of different treatment strategies have been published in the literature, without any comparative studies. METHODS: Our aim was to describe the current international practice variation surrounding pharmacological treatment currently being employed to treat paradoxical hypertension following the repair of coarctation of the aorta in children...
May 2017: World Journal for Pediatric & Congenital Heart Surgery
https://www.readbyqxmd.com/read/28502064/optimization-of-water-oil-surfactant-system-for-preparation-of-medium-chain-length-poly-3-hydroxyalkanoates-mcl-pha-incorporated-nanoparticles-via-nanoemulsion-templating-technique
#6
K A Ishak, M Suffian M Annuar, N Ahmad
Polymeric nanoparticles gain a widespread interest in food and pharmaceutical industries as delivery systems that encapsulate, protect, and release lipophilic compounds such as omega-3 fatty acids, fat-soluble vitamins, carotenoids, carvedilol, cyclosporine, and ketoprofen. In this study, medium-chain-length poly-3-hydroxyalkanoate (mcl-PHA)-incorporated nanoparticle was developed via facile organic solvent-free nanoemulsion templating technique. The water content (W/surfactant-to-oil (S/O)), S/O, and Cremophor EL-to-Span 80 (Cremo/Sp80) ratios were first optimized using response surface methodology (RSM) to obtain nanoemulsion template prior to incorporation of mcl-PHA...
May 13, 2017: Applied Biochemistry and Biotechnology
https://www.readbyqxmd.com/read/28495583/application-of-miscibility-analysis-and-determination-of-soluplus-solubility-map-for-development-of-carvedilol-loaded-nanofibers
#7
Olivera Kaljević, Jelena Djuris, Bojan Čalija, Zoran Lavrič, Julijana Kristl, Svetlana Ibrić
Electrospinning was used to produce carvedilol-loaded Soluplus polymer nanofibers using a systematic approach. Miscibility between drug and polymer was determined through calculation of the interaction parameter, χ, and the difference between the total solubility parameters, Δdt. A solubility map for Soluplus was obtained by examining different solvent systems, carrying out electrospinning, and characterizing the nanofibers formed. Miscibility studies showed that carvedilol and Soluplus can form a miscible system (χ=-2...
May 8, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28491305/effects-of-carvedilol-on-structural-and-functional-outcomes-and-plasma-biomarkers-in-the-mouse-transverse-aortic-constriction-heart-failure-model
#8
Caryn Hampton, Raymond Rosa, Daphne Szeto, Gail Forrest, Barry Campbell, Richard Kennan, Shubing Wang, Chin-Hu Huang, Loise Gichuru, Xiaoli Ping, Xiaolan Shen, Kersten Small, Jeffrey Madwed, Joseph J Lynch
INTRODUCTION: Despite the widespread use of the mouse transverse aortic constriction heart failure model, there are no reports on the characterization of the standard-of-care agent carvedilol in this model. METHODS: Left ventricular pressure overload was produced in mice by transverse aortic constriction between the innominate and left common carotid arteries. Carvedilol was administered at multiple dose levels (3, 10 and 30 mg/kg/day per os; yielding end-study mean plasma concentrations of 0...
2017: SAGE Open Medicine
https://www.readbyqxmd.com/read/28472245/beta-blocker-subtype-and-risks-of-perioperative-adverse-events-following-non-cardiac-surgery-a-nationwide-cohort-study
#9
Mads E Jørgensen, Robert D Sanders, Lars Køber, Kala Mehta, Christian Torp-Pedersen, Mark A Hlatky, Jannik L Pallisgaard, Richard E Shaw, Gunnar H Gislason, Per F Jensen, Charlotte Andersson
Aims: Beta-blockers vary in pharmacodynamics and pharmacokinetic properties. It is unknown whether specific types are associated with increased perioperative risks. We evaluated perioperative risks associated with beta-blocker subtypes, overall and in patient subgroups. Methods and results: We performed a Danish Nationwide cohort study, 2005-2011, of patients treated chronically with beta blocker (atenolol, bisoprolol, carvedilol, metoprolol, propranolol, or other) prior to non-cardiac surgery...
May 2, 2017: European Heart Journal
https://www.readbyqxmd.com/read/28471055/a-novel-in-situ-strategy-for-the-preparation-of-a-%C3%AE-cyclodextrin-polydopamine-coated-capillary-column-for-capillary-electrochromatography-enantioseparations
#10
Heying Guo, Xiaoying Niu, Congjie Pan, Tao Yi, Hongli Chen, Xingguo Chen
Inspired by the chiral recognition ability of β-cyclodextrin and the natural adhesive properties of polydopamine under alkaline conditions, in this study, a rapid and in situ modification strategy was developed to fabricate β-cyclodextrin/polydopamine composite material coated-capillary columns for open tubular capillary electrochromatography. The results of scanning electron microscopy, FTIR spectroscopy, streaming potential and electro-osmotic flow studies indicated that β-cyclodextrin/polydopamine was successfully fixed on the inner wall of the capillary column...
May 4, 2017: Journal of Separation Science
https://www.readbyqxmd.com/read/28469221/did-carvedilol-really-have-more-severe-adverse-events-than-propranolol-in-cirrhotic-patients
#11
Gin-Ho Lo
No abstract text is available yet for this article.
May 2017: American Journal of Gastroenterology
https://www.readbyqxmd.com/read/28444654/digoxin-toxicity-in-a-neonate-caused-by-the-interaction-with-carvedilol
#12
Alexia Moser-Bracher, Christian Balmer, Anna Cavigelli, Aylin Satir, Angela Caduff Good, Dietrich Klauwer
No abstract text is available yet for this article.
March 2017: Klinische Pädiatrie
https://www.readbyqxmd.com/read/28435058/in-vitro-and-in-vivo-evaluation-of-gastro-retentive-carvedilol-loaded-chitosan-beads-using-gastroplus%C3%A2
#13
Radhakrishnan Praveen, Priya Ranjan Prasad Verma, Jayachandran Venkatesan, Dong-Han Yoon, Se-Kwon Kim, Sandeep Kumar Singh
The objective of present investigation was to develop gastro-retentive controlled release system of carvedilol using biological macromolecule, chitosan. 3(2) full factorial design was adopted for optimization of tripolyphosphate (X1) and curing time (X2). Bead stability in 0.1N HCl, buoyancy duration, density, drug loading, dissolution efficiency and cumulative percentage release at 8th hour were evaluated as dependent variables. The levels of X1 and X2 of optimized formulation having maximum desirability was found to 2...
April 20, 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/28434020/bisoprolol-compared-with-carvedilol-and-metoprolol-succinate-in-the-treatment-of-patients-with-chronic-heart-failure
#14
Hanna Fröhlich, Lorella Torres, Tobias Täger, Dieter Schellberg, Anna Corletto, Syed Kazmi, Kevin Goode, Morten Grundtvig, Torstein Hole, Hugo A Katus, John G F Cleland, Dan Atar, Andrew L Clark, Stefan Agewall, Lutz Frankenstein
AIMS: Beta-blockers are recommended for the treatment of chronic heart failure (CHF). However, it is disputed whether beta-blockers exert a class effect or whether there are differences in efficacy between agents. METHODS AND RESULTS: 6010 out-patients with stable CHF and a reduced left ventricular ejection fraction prescribed either bisoprolol, carvedilol or metoprolol succinate were identified from three registries in Norway, England, and Germany. In three separate matching procedures, patients were individually matched with respect to both dose equivalents and the respective propensity scores for beta-blocker treatment...
April 22, 2017: Clinical Research in Cardiology: Official Journal of the German Cardiac Society
https://www.readbyqxmd.com/read/28432614/dual-activity-of-hydroxypropyl-%C3%AE-cyclodextrin-and-water-soluble-carriers-on-the-solubility-of-carvedilol
#15
Abdelmoumin Zoghbi, Tianjiao Geng, Bo Wang
Carvedilol (CAR) is a non-selective α and β blocker categorized as class II drug with low water solubility. Several recent studies have investigated ways to overcome this problem. The aim of the present study was to combine two of these methods: the inclusion complex using hydroxypropyl-β-cyclodextrin (HPβCD) with solid dispersion using two carriers: Poloxamer 188 (PLX) and Polyvinylpyrrolidone K-30 (PVP) to enhance the solubility, bioavailability, and the stability of CAR. Kneading method was used to prepare CAR-HPβCD inclusion complex (KD)...
April 21, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28417439/clinical-pharmacokinetics-of-sacubitril-valsartan-lcz696-a-novel-angiotensin-receptor-neprilysin-inhibitor
#16
REVIEW
Surya Ayalasomayajula, Thomas Langenickel, Parasar Pal, Sreedevi Boggarapu, Gangadhar Sunkara
Sacubitril/valsartan (LCZ696) is indicated for the treatment of heart failure with reduced ejection fraction. Absorption of sacubitril/valsartan and conversion of sacubitril (prodrug) to sacubitrilat (neprilysin inhibitor) was rapid with maximum plasma concentrations of sacubitril, sacubitrilat, and valsartan (angiotensin receptor blocker) reaching within 0.5, 1.5-2.0, and 2.0-3.0 h, respectively. With a two-fold increase in dose, an increase in the area under the plasma concentration-time curve was proportional for sacubitril, ~1...
April 17, 2017: Clinical Pharmacokinetics
https://www.readbyqxmd.com/read/28410967/involvement-of-alpha-and-beta-adrenoceptors-in-the-automaticity-of-the-isolated-guinea-pig-pulmonary-vein-myocardium
#17
Masahiko Irie, Yayoi Tsuneoka, Mariko Shimobayashi, Nao Hasegawa, Yusuke Tanaka, Soh Mochizuki, Sho Ichige, Shogo Hamaguchi, Iyuki Namekata, Hikaru Tanaka
We examined the involvement of adrenoceptors in the automaticity of the pulmonary vein myocardium, which probably plays a crucial role in the generation of atrial fibrillation. The automatic activity of the myocardium in guinea pig pulmonary vein tissue preparations were monitored by contractile force or membrane potential measurement. In quiescent preparations, application of noradrenaline induced an automatic activity. The firing frequency was reduced by prazosin or atenolol. Methoxamine induced an automatic activity of low frequency, which was accelerated by further application of isoproterenol...
April 2017: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/28410843/left-ventricular-hypertrophy-does-not-prevent-heart-failure-in-experimental-hypertension
#18
H Hernán Gómez Llambí, G Cao, M Donato, D Suárez, G Ottaviano, A Müller, B Buchholz, R Gelpi, M Otero-Losada, J Milei
BACKGROUND: Left ventricular hypertrophy (LVH) secondary to hypertension has been accepted to prevent heart failure (HF) while paradoxically increasing cardiovascular morbi-mortality. OBJECTIVES: To evaluate whether antihypertensive treatment inhibits LVH, restores beta-adrenergic response and affects myocardial oxidative metabolism. METHODS: Ninety spontaneously hypertensive rats (SHR) were distributed into groups and treated (mg/kg, p.o...
March 27, 2017: International Journal of Cardiology
https://www.readbyqxmd.com/read/28399647/%C3%AE-blockers-cocaine-and-the-unopposed-%C3%AE-stimulation-phenomenon
#19
John R Richards, Judd E Hollander, Edward A Ramoska, Fareed N Fareed, I Charles Sand, María Manuela Izquierdo Gómez, Richard A Lange
Cocaine abuse remains a significant worldwide health problem. Patients with cardiovascular toxicity from cocaine abuse frequently present to the emergency department for treatment. These patients may be tachycardic, hypertensive, agitated, and have chest pain. Several pharmacological options exist for treatment of cocaine-induced cardiovascular toxicity. For the past 3 decades, the phenomenon of unopposed α-stimulation after β-blocker use in cocaine-positive patients has been cited as an absolute contraindication, despite limited and inconsistent clinical evidence...
May 2017: Journal of Cardiovascular Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/28396867/carvedilol-attenuates-the-progression-of-hepatic-fibrosis-induced-by-bile-duct-ligation
#20
Xiaopeng Tian, Chunhong Zhao, Jinbo Guo, Shurui Xie, Fengrong Yin, Xiaoxia Huo, Xiaolan Zhang
Background. The sympathetic nervous system (SNS) is responsible for hepatic stellate cells (HSCs) activation and the accumulation of collagen that occurs in hepatic fibrogenesis. Carvedilol has been widely used for the complication of hepatic cirrhosis in the clinic. Furthermore, it has powerful antioxidant properties. We assessed the potential antifibrotic effects of carvedilol and the underlying mechanisms that may further enhance its clinical benefits. Methods. Using a bile duct ligation rat model of hepatic fibrosis, we studied the effects of carvedilol on the fibrosis, collagen deposition, and oxidative stress based on histology, immunohistochemistry, western blot, and RT-PCR analyses...
2017: BioMed Research International
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