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https://www.readbyqxmd.com/read/28286117/carvedilol-prevents-functional-deficits-in-peripheral-nerve-mitochondria-of-rats-with-oxaliplatin-evoked-painful-peripheral-neuropathy
#1
Aparna Areti, Prashanth Komirishetty, Ashutosh Kumar
Oxaliplatin use as chemotherapeutic agent is frequently limited by cumulative neurotoxicity which may compromise quality of life. Reports relate this neurotoxic effect to oxidative stress and mitochondrial dysfunction in peripheral nerves and dorsal root ganglion (DRG). Carvedilol is an antihypertensive drug, has also been appreciated for its antioxidant and mitoprotective properties. Carvedilol co-treatment did not reduce the anti-tumor effects of oxaliplatin in human colon cancer cells (HT-29), but exhibited free radical scavenging activity against oxaliplatin-induced oxidative stress in neuronal cells (Neuro-2a)...
March 9, 2017: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/28266722/development-and-validation-of-a-hplc-uv-method-for-the-simultaneous-determination-of-the-antipsychotics-clozapine-olanzapine-and-quetiapine-several-beta-blockers-and-their-metabolites
#2
Margarete Silva Gracia, Alexandra Köppl, Sandra Unholzer, Ekkehard Haen
A simple, accurate and selective column-switching high performance liquid chromatography (HPLC) method was developed and validated for simultaneous quantification of six beta-blockers (metoprolol MET, timolol TIM, bisoprolol BIS, propranolol PRO, carvedilol CAR and nebivolol NEB), three of their metabolites (α-hydroxy metoprolol α-HMET, N-desisopropyl propranolol DIPRO and 4'-hydroxy carvedilol 4-HCAR), three antipsychotics (olanzapine OLA, clozapine CLO and quetiapine QUE) and three of their metabolites (N-desmethyl olanzapine DMOLA, N-desmethyl clozapine DMCLO and N-desalkyl quetiapine DAQUE) in human serum...
March 7, 2017: Biomedical Chromatography: BMC
https://www.readbyqxmd.com/read/28261384/addition-of-simvastatin-to-carvedilol-non-responders-a-new-pharmacological-therapy-for-treatment-of-portal-hypertension
#3
Zeeshan Ahmad Wani, Sonmoon Mohapatra, Afaq Ahmad Khan, Ashutosh Mohapatra, Ghulam Nabi Yatoo
AIM: To determine whether addition of simvastatin could be an important pharmacological rescue therapy for carvedilol non-responders. METHODS: One hundred and two consecutive patients of cirrhosis of liver with significant portal hypertension were included. Hepatic venous pressure gradient (HVPG) was measured at the base line and after proper optimization of dose; chronic response was assessed at 3 mo. Carvedilol non-responders were given simvastatin 20 mg per day (increased to 40 mg per day at day 15)...
February 18, 2017: World Journal of Hepatology
https://www.readbyqxmd.com/read/28244261/effect-of-beta-adrenergic-blockade-with-carvedilol-on-cachexia-in-severe-chronic-heart-failure-results-from-the-copernicus-trial
#4
Andrew L Clark, Andrew J S Coats, Henry Krum, Hugo A Katus, Paul Mohacsi, Damien Salekin, Melissa K Schultz, Milton Packer, Stefan D Anker
BACKGROUND: Cardiac cachexia frequently accompanies the progression of heart failure despite the use of effective therapies for left ventricular dysfunction. Activation of the sympathetic nervous system has been implicated in the pathogenesis of weight loss, but the effects of sympathetic antagonism on cachexia are not well defined. METHODS: We prospectively evaluated changes in body weight in 2289 patients with heart failure who had dyspnoea at rest or on minimal exertion and a left ventricular ejection fraction <25%...
February 27, 2017: Journal of Cachexia, Sarcopenia and Muscle
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
#5
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/28225060/new-limits-of-secondary-%C3%AE-relaxation
#6
Satya N Tripathy, Marzena Rams-Baron, Zaneta Wojnarowska, Justyna Knapik-Kowalczuk, Marian Paluch
Glass is an ultraviscous liquid that ceases to flow on a laboratory timescale but continues to relax on a geological timescale. Quintessentially, it has become hopeless for humans to explore the equilibrium behavior of glass, although the technology of glass making witness a remarkable advance. In this work, we propose a novel thermodynamic path to prepare a high density amorphous state of matter (carvedilol dihydrogen phosphate) using high pressure. In addition, we provide the impeccable experimental evidence of heterogeneous nature of secondary β-relaxation and probe its properties to understand the various aspects of pressure densified glass, such as dynamics, packing and disorder...
February 22, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28213164/carvedilol-use-is-associated-with-improved-survival-in-patients-with-liver-cirrhosis-and-ascites
#7
Rohit Sinha, Khalida A Lockman, Nethmee Mallawaarachchi, Marcus Robertson, John N Plevris, Peter C Hayes
BACKGROUND & AIMS: Carvedilol, a non-selective beta-blocker (NSBB) with additional anti-alpha 1 receptor activity, is a potent portal hypotensive agent and has been used as prophylaxis against variceal bleeding. However, its safety in patients with decompensated liver cirrhosis and ascites is still disputed. In this study, we examined whether long-term use of carvedilol in patients with ascites is a risk factor for mortality. METHODS: A single-centre retrospective analysis of 325 consecutive patients with liver cirrhosis and ascites presenting to our Liver Unit between 1st of January 2009 to 31st August 2012 was carried out...
February 16, 2017: Journal of Hepatology
https://www.readbyqxmd.com/read/28211304/granisetron-and-carvedilol-can-protect-experimental-rats-againstadjuvant-induced-arthritis
#8
Yasmin Moustafa Ahmed, Basim Anwar Shehata Messiha, Ali Ahmed Abo-Saif
CONTEXT: Rheumatoid arthritis (RA), a disabling autoimmune disorder of the joints as well as other organs, affects about 1% of population. Unfortunately, all current treatments of RA cause severe gastrointestinal, renal and other complications. OBJECTIVE: We aimed to evaluate the possible antiarthritic effects of a serotonin 5-HT3 receptor blocker, granisetron, and a nonselective adrenergic receptor blocker, carvedilol, on complete Freund's adjuvant-induced RA in adult female albino rats...
April 2017: Immunopharmacology and Immunotoxicology
https://www.readbyqxmd.com/read/28188000/effectiveness-of-a-management-program-for-outpatient-clinic-or-remote-titration-of-beta-blockers-in-crt-patients-the-restore-study
#9
Antonio D'Onofrio, Pietro Palmisano, Antonio Rapacciuolo, Ernesto Ammendola, Leonardo Calò, Antonio Ruocco, Valter Bianchi, Fabio Maresca, Giuseppe Del Giorno, Annamaria Martino, Ciro Mauro, Monica Campari, Sergio Valsecchi, Michele Accogli
BACKGROUND: Many patients fail to receive β-blockers before cardiac resynchronization therapy defibrillator (CRT-D) implantation, or receive them at a suboptimal dose, and require optimization after implantation. We assessed the effectiveness of a structured program for β-blocker titration in CRT-D patients followed up by means of conventional in-clinic visits or remote monitoring. METHODS AND RESULTS: 130 patients undergoing CRT implantation and treated according to the standard practice of the centers were included as a control group...
February 5, 2017: International Journal of Cardiology
https://www.readbyqxmd.com/read/28185991/formulation-and-characterization-of-nanofibers-and-films-with-carvedilol-prepared-by-electrospinning-and-solution-casting-method
#10
Marko Krstić, Marija Radojević, Dušica Stojanović, Vesna Radojević, Petar Uskoković, Svetlana Ibrić
The preparation and characterization of films and nanofibers with carvedilol as a poorly water-soluble drug in poly (ethylene oxide) (PEO) polymer were investigated. Films are prepared by solution casting method, and nanofibers by electrospinning from a polymer solution. Water and mixture of ethanol and water were used as solvents. FT-IR analysis of the samples showed that there was no interaction between the polymer and the drug substance. DSC analysis revealed that carvedilol was dissolved in the polymer and influenced the degree of crystallinity of PEO...
April 1, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28181117/cyp2d6-genetic-variation-and-beta-blocker-maintenance-dose-in-patients-with-heart-failure
#11
Jasmine A Luzum, Kevin M Sweet, Philip F Binkley, Tara J Schmidlen, Joseph P Jarvis, Michael F Christman, Wolfgang Sadee, Joseph P Kitzmiller
PURPOSE: This study examined whether a CYP2D6 polymorphism (CYP2D6*4) was related to beta-blocker maintenance dose in patients with heart failure. METHODS: Logistic regression modeling was utilized in a retrospective chart-review analysis of heart-failure patients (60% Male, 90% of European descent) to assess whether CYP2D6*4 (non-functional CYP2D6 allele present in 1 of 5 individuals of European descent) is associated with maintenance dose of carvedilol (n = 65) or metoprolol (n = 33)...
February 8, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28155135/influence-of-peroxide-impurities-in-povidone-on-the-stability-of-selected-%C3%AE-blockers-with-the-help-of-hplc
#12
Saklecha Prachi, Chaudhary Komal, Mehta J Priti
A present study was conducted to investigate compatibility of β-blocker drugs( like atenolol, labetalol hydrochloride, bisoprolol fumarate, metoprolol succinate, carvedilol and propranolol hydrochloride) with the pharmaceutical excipient povidone. To check the influence of peroxide impurity present in povidone on the stability of β-blockers, a binary mixture technique has been adopted. The binary mixtures (1:1) of β-blockers with povidone excipient were stored for the duration of 6 months at accelerated conditions (40°C and 75% RH) and analyzed with the technique of high-performance liquid chromatography (HPLC)...
February 2, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28141699/cardioprotective-effects-of-carvedilol-in-inhibiting-doxorubicin-induced-cardiotoxicity
#13
Maryam Nabati, Ghasem Janbabai, Saideh Baghyari, Maryam Esmaili, Jamshid Yazdani
PURPOSE: Anthracyclines (ANTs) are a class of active anti-neoplastic agents with topoisomerase-interacting activity that are considered the most active agents for the treatment of breast cancer. We investigated the efficacy of carvedilol in the inhibition of ANT-induced cardiotoxicity. METHODS: In this randomized, single-blind, placebo-controlled study, 91 women with recently diagnosed breast cancer undergoing ANT therapy were randomly assigned to groups treated with either carvedilol (n=46) or placebo (n=45)...
January 30, 2017: Journal of Cardiovascular Pharmacology
https://www.readbyqxmd.com/read/28119104/carvedilol-loaded-nanocapsules-mucoadhesive-properties-and-permeability-across-the-sublingual-mucosa
#14
Paula Dos Santos Chaves, Aline Ferreira Ourique, Luiza Abrahão Frank, Adriana Raffin Pohlmann, Sílvia Stanisçuaski Guterres, Ruy Carlos Ruver Beck
Carvedilol is a drug used to treat heart failure, hypertension, and coronary artery diseases . However, it has low oral bioavailability (25-35%) due to its high first-pass hepatic metabolism. The objective of this study was to develop carvedilol-loaded mucoadhesive nanocapsules as delivery systems for the sublingual administration of the drug. Nanocapsules were prepared using poly(ε-caprolactone) (CAR-LNC) and Eudragit® RS 100 (CAR-NC) as polymeric wall. In vitro interaction of formulations with mucin was performed to predict their mucoadhesion capacity...
January 21, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28114735/effects-of-type-2-diabetes-mellitus-in-patients-on-treatment-with-glibenclamide-and-metformin-on-carvedilol-enantiomers-metabolism
#15
Glauco H B Nardotto, Eduardo B Coelho, Carlos E Paiva, Vera L Lanchote
Carvedilol is available in clinical practice as a racemate in which (S)-(-)-carvedilol is a β- and α1 -adrenergic antagonist and (R)-(+)-carvedilol is only an α1 -adrenergic antagonist. Carvedilol is mainly metabolized by glucuronidation, by CYP2D6 to hydroxyphenylcarvedilol (OHC), and by CYP2C9 to O-desmethylcarvedilol (DMC). This study evaluated the pharmacokinetics of carvedilol enantiomers and their metabolites OHC and DMC in healthy volunteers (n = 13) and in type 2 diabetes mellitus patients with good glycemic control (n = 13)...
January 23, 2017: Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28099882/the-35-year-odyssey-of-beta-blockers-in-cirrhosis-any-gender-difference-in-sight
#16
REVIEW
Maria Antonella Burza, Hanns-Ulrich Marschall, Laura Napoleone, Antonio Molinaro
Cirrhosis is the end-stage of chronic liver disease and leads to the development of portal hypertension and its complications such as esophagogastric varices. Non-selective beta blockers (NSBB) are the keystone for the treatment of portal hypertension since the 1980s and, over the decades, several studies have confirmed their beneficial effect on the prevention of variceal (re)bleeding. Pharmacological studies showed effects of gender, sex hormones, oral contraceptives, and pregnancy on cytochrome P450 (CYPs) enzymes that metabolise NSBB, suggesting that gender differences might exist in the effect of NSBB...
January 15, 2017: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
https://www.readbyqxmd.com/read/28087848/correction-to-early-administration-of-carvedilol-protected-against-doxorubicin-induced-cardiomyopathy
#17
(no author information available yet)
No abstract text is available yet for this article.
February 2017: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/28073770/impact-of-beta-blocker-initiation-timing-on-mortality-risk-in-patients-with-diabetes-mellitus-undergoing-noncardiac-surgery-a-nationwide-population-based-cohort-study
#18
Ray-Jade Chen, Hsi Chu, Lung-Wen Tsai
BACKGROUND: Relevant clinical studies have been small and have not convincingly demonstrated whether the perioperative initiation of beta-blockers should be considered in patients with diabetes mellitus undergoing noncardiac surgery. METHODS AND RESULTS: In this nationwide propensity score-matched study, we included patients with diabetes mellitus undergoing noncardiac surgery between 2000 and 2011 from Taiwan's National Health Insurance Research Database. Patients were classified as beta-blocker and non-beta-blocker cohorts...
January 10, 2017: Journal of the American Heart Association
https://www.readbyqxmd.com/read/28069789/hypotension-induced-by-the-concomitant-use-of-a-calcium-channel-blocker-and-clarithromycin
#19
Sayako Takeuchi, Yuki Kotani, Toshihide Tsujimoto
In the elderly, calcium-channel blockers are the first-line treatment for hypertension, and macrolides are commonly prescribed antibiotics. Here we report a 78-year-old man taking nifedipine, diltiazem and carvedilol who presented with persistent hypotension and bradycardia after clarithromycin was prescribed. He was diagnosed with drug-induced hypotension and treated with fluid resuscitation and vasoactive agents. His symptoms gradually improved. He was transferred out of the intensive care unit 3 days after hospitalisation...
January 9, 2017: BMJ Case Reports
https://www.readbyqxmd.com/read/28064425/enantioselective-resolution-of-r-s-carvedilol-to-s-carvedilol-by-biocatalysts
#20
Swetha Ettireddy, Vijitha Chandupatla, Ciddi Veeresham
Among the microorganisms employed in the study, Aspergillus niger (GUFCC5443), Escherichia coli (ATCC9637), Streptomyces halstedii (CKM-2), Pseudomonas putida (NCIB9494), Cunninghamella elegans (NCIM689) and Sphingomonas paucimobilis (NCTC11030) were capable for the enantioselective conversion of racemic Carvedilol. Immobilization technique enhanced the enantioselectivity of microorganisms and thus increased the enantiomeric purity of the drug. Excellent enantiomeric ratios (E) were found in reactions catalyzed by immobilized A...
February 2017: Natural Products and Bioprospecting
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