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Tetsuro Tsujimoto, Hiroshi Kajio, Martin F Shapiro, Takehiro Sugiyama
OBJECTIVE: To assess the relationship between use of β-blockers and all-cause mortality in patients with and without diabetes. PATIENTS AND METHODS: Using data from the US National Health and Nutrition Examination Survey 1999-2010, we conducted a prospective cohort study. The study participants were followed-up from the survey participation date until December 31, 2011. We used a Cox proportional hazards model for all-cause mortality analysis. The multivariate-adjusted hazard ratios (HRs) of the participants taking β-blockers were compared with those of the participants not taking β-blockers...
March 9, 2018: Mayo Clinic Proceedings
Monica Samuel Avila, Silvia Moreira Ayub-Ferreira, Mauro Rogerio de Barros Wanderley Junior, Fatima das Dores Cruz, Sara Michelly Gonçalves Brandão, Vagner Oliveira Carvalho Rigaud, Marilia Higushi-Dos-Santos, Ludhmila Abrahão Hajjar, Roberto Kalil Filho, Paulo Marcelo Hoff, Marina Sahade, Marcela S M Ferrari, Romulo Leopoldo de Paula Costa, Max Senna Mano, Cecilia Beatriz Bittencourt Viana Cruz, Maria Cristina Abduch, Marco Stephan Lofrano Alves, Guilherme Veiga Guimaraes, Victor Sarli Issa, Marcio Sommer Bittencourt, Edimar Alcides Bocchi
BACKGROUND: Anthracycline (ANT) chemotherapy is associated with cardiotoxicity. Prevention with β-blockers remains controversial. OBJECTIVE: The aim of this prospective, randomized, double-blind, placebo-controlled study was to evaluate the role of carvedilol in preventing ANT cardiotoxicity. METHODS: We randomized 200 patients with HER2-negative breast cancer tumor status and normal left ventricular ejection fraction (LVEF) referred for ANT (240 mg/m2 ) to receive carvedilol or placebo until chemotherapy completion...
March 3, 2018: Journal of the American College of Cardiology
Alvin Tieu, Thomas J Velenosi, Andrew S Kucey, Matthew A Weir, Bradley L Urquhart
BACKGROUND AND OBJECTIVES: There is a paucity of data available to describe drug dialyzability. Of the available information, most was obtained before implementation of modern hemodialysis membranes. Our study characterized dialyzability of the most commonly prescribed β -blockers in patients undergoing high-flux hemodialysis. DESIGN, SETTING, PARTICIPANTS, & MEASUREMENTS: Patients on hemodialysis ( n =8) were recruited to an open label, pharmacokinetic, four-way crossover trial...
March 8, 2018: Clinical Journal of the American Society of Nephrology: CJASN
Saša Kajdič, Franc Vrečer, Petra Kocbek
Polymer nanofibers have become increasingly important for improvement of dissolution and bioavailability of poorly soluble drugs, representing a great challenge in pharmaceutical development. Here, we introduced a new concept of using amphiphilic polymers as fundamental excipients in electrospun nanofibers, which would improve drug solubilization and accelerate its release. Hydrophilic poloxamer-based nanofibers were developed as a novel drug delivery system for carvedilol. These nanofibers were electrospun from different liquid carvedilol dispersions, as carvedilol (nano)suspensions or ethanol solution...
March 4, 2018: European Journal of Pharmaceutical Sciences
R Schwarzer, D Kivaranovic, R Paternostro, M Mandorfer, T Reiberger, M Trauner, M Peck-Radosavljevic, A Ferlitsch
BACKGROUND: Sequential measurements of hepatic venous pressure gradient (HVPG) are used to assess the haemodynamic response to nonselective betablockers (NSBBs) in patients with portal hypertension. AIMS: To assess the rates of HVPG response to different doses of carvedilol. METHODS: Consecutive patients with cirrhosis undergoing HVPG-guided carvedilol therapy for primary prophylaxis of variceal bleeding between 08/2010 and 05/2015 were retrospectively included...
February 28, 2018: Alimentary Pharmacology & Therapeutics
Sin Young Choi, Hae Jin Kee, Li Jin, Yuhee Ryu, Simei Sun, Gwi Ran Kim, Myung Ho Jeong
Histone deacetylase (HDAC) inhibitors are gaining increasing attention as potential therapeutics for cardiovascular diseases as well as cancer. We recently reported that the class II HDAC inhibitor, MC1568, and the phytochemical, gallic acid, lowered high blood pressure in mouse models of hypertension. We hypothesized that class II HDACs may be involved in the regulation of hypertension. The aim of this study was to determine and compare the effects of well-known HDAC inhibitors (TMP269, panobinostat, and MC1568), phytochemicals (gallic acid, sulforaphane, and piceatannol), and anti-hypertensive drugs (losartan, carvedilol, and furosemide) on activities of class IIa HDACs (HDAC4, 5, 7, and 9)...
February 23, 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
Luis Antonio D Silva, Susana L Almeida, Ellen C P Alonso, Priscila B R Rocha, Felipe T Martins, Luís A P Freitas, Stephania F Taveira, Marcilio S S Cunha-Filho, Ricardo N Marreto
Hot-melt extrusion (HME) has gained increasing attention in the pharmaceutical industry; however, its potential in the preparation of solid self-emulsifying drug delivery systems (S-SMEDDS) is still unexplored. This study sought to prepare enteric S-SMEDDS by HME and evaluate the effects of the process and formulation variables on S-SMEDDS properties via Box-Behnken design. Liquid SMEDDS were developed, and carvedilol was used as a class II model drug. Mean size, polydispersity index (PdI) and zeta potential of the resulting microemulsions were determined...
February 16, 2018: International Journal of Pharmaceutics
Lindsey R Sangaralingham, S Jeson Sangaralingham, Nilay D Shah, Xiaoxi Yao, Shannon M Dunlay
BACKGROUND: The US Food and Drug Administration approved the use of sacubitril/valsartan in patients with heart failure with reduced ejection fraction in July 2015. We aimed to assess the adoption and prescription drug costs of sacubitril/valsartan in its first 18 months after Food and Drug Administration approval. METHODS AND RESULTS: Using a large US insurance database, we identified privately insured and Medicare Advantage beneficiaries who filled a first prescription for sacubitril/valsartan between July 1, 2015, and December 31, 2016...
February 2018: Circulation. Heart Failure
João Pedro Ferreira, Nicolas Girerd, John Gregson, Ichraq Latar, Abhinav Sharma, Marc A Pfeffer, John J V McMurray, Azmil H Abdul-Rahim, Bertram Pitt, Kenneth Dickstein, Patrick Rossignol, Faiez Zannad
BACKGROUND: Stroke can occur after myocardial infarction (MI) in the absence of atrial fibrillation (AF). OBJECTIVES: This study sought to identify risk factors (excluding AF) for the occurrence of stroke and to develop a calibrated and validated stroke risk score in patients with MI and heart failure (HF) and/or systolic dysfunction. METHODS: The datasets included in this pooling initiative were derived from 4 trials: CAPRICORN (Effect of Carvedilol on Outcome After Myocardial Infarction in Patients With Left Ventricular Dysfunction), OPTIMAAL (Optimal Trial in Myocardial Infarction With Angiotensin II Antagonist Losartan), VALIANT (Valsartan in Acute Myocardial Infarction Trial), and EPHESUS (Eplerenone Post-Acute Myocardial Infarction Heart Failure Efficacy and Survival Study); EPHESUS was used for external validation...
February 20, 2018: Journal of the American College of Cardiology
Djordje Medarević, Jelena Djuriš, Svetlana Ibrić, Miodrag Mitrić, Kyriakos Kachrimanis
The aim of this study is to develop nanosuspension of carvedilol (CRV) by wet media milling. Concentration of polymeric stabilizer (hydroxypropyl cellulose-HPC-SL), milling speed and size of milling beads were identified as critical formulation and process parameters and their effect on CRV particle size after 60 min of milling was assessed using a Box-Behnken experimental design. Optimized nanosuspension was solidified using spray drying and freeze drying and subjected to solid state characterization. Low stabilizer concentration (10%), low milling speed (300 rpm) with small milling beads (0...
February 10, 2018: International Journal of Pharmaceutics
Jia Liu, Min Wang
Mutations in amyloid precursor protein (APP) and presenilin1 result in overproduction and accumulation of β-amyloid (Aβ) peptide, which has been shown to play an important role in Alzheimer's disease (AD) pathogenesis. Carvedilol, a nonselective β-adrenergic receptor blocker used for treatment for heart failure and hypertension, has displayed its neuroprotective capacity due to its antioxidant property. In this study, we investigated whether Carvedilol has a neuronal protective effect against endogenous Aβ neurotoxicity in mouse Neuro2a (N2a) cells transfected with Swedish amyloid precursor protein (Swe-APP) mutant and Presenilin exon9 deletion mutant (N2a/Swe...
February 12, 2018: Cell Stress & Chaperones
Dong-Ju Choi, Chan Soon Park, Jin Joo Park, Hae-Young Lee, Seok-Min Kang, Byung-Su Yoo, Eun-Seok Jeon, Seok Keun Hong, Joon-Han Shin, Myung-A Kim, Dae-Gyun Park, Eung-Ju Kim, Soon-Jun Hong, Seok Yeon Kim, Jae-Joong Kim
BACKGROUND: Carvedilol is a non-selective, third-generation beta-blocker and is one of the cornerstones for treatment for patients with heart failure and reduced ejection fraction (HFrEF). However, due to its short half-life, immediate-release carvedilol (IR) needs to be prescribed twice a day. Recently, slow-release carvedilol (SR) has been developed. The aim of this study is to evaluate whether carvedilol-SR is non-inferior to standard carvedilol-IR in terms of its clinical efficacy in patients with HFrEF...
February 13, 2018: Trials
Ansha Subramanian, Mangaiarkkarasi Adhimoolam, Suresh Kannan
Aim: Drug-drug interactions (DDIs) are one of the major but preventable cause of adverse drug reaction. Study of prevalence and prediction of DDIs will make the physician easier to provide better patient care and mitigate patient's harm. Hence, the study was planned to evaluate the potential DDIs among medication prescribed to hypertensive patients in our hospital. Materials and Methods: A prospective, cross-sectional study was conducted among the hypertensive patients in medicine (outpatient/inpatient) department over the period of three months in a tertiary care hospital...
January 2018: Perspectives in Clinical Research
Abidemi J Akindele, Gabriel O Oludadepo, Kennedy I Amagon, Dhirendra Singh, Daniel D Osiagwu
This study investigated the protective effects of carvedilol alone and coadministered with prednisolone and diltiazem on doxorubicin (DOX) and 5-fluorouracil (5-FU)-induced toxicity. Each of 2 pools of 70 female rats were randomly allotted into 10 groups of 7 animals each and treated as follows: Group 1: normal saline (10 mL/kg); Group 2: normal saline and DOX (40 mg/kg)/5-FU (20 mg/kg) alone; Group 3: gallic acid (200 mg/kg) and DOX/5-FU; Group 4: carvedilol (0.075 mg/kg) and DOX/5-FU; Group 5: carvedilol (0...
February 2018: Pharmacology Research & Perspectives
Masahiro Iwaki, Toshiro Niwa, Yukiko Nakamura, Atsushi Kawase, Hiroshi Komura
The relative contribution of cytochrome P450 (CYP) isoforms responsible for carvedilol (CAR) oxidation in rats were evaluated in order to compare with that of reported human CYPs responsible for the metabolism of CAR enantiomers. The depletion of CAR enantiomers by recombinant CYPs and the effects of CYP-selective inhibitors on the depletion catalyzed by rat liver microsomes (RLM) was determined. Quinine (rat CYP2D inhibitor) markedly inhibited the metabolism of both R- and S-CAR by RLM. The metabolism of S-CAR was inhibited more than that of R-CAR by furafylline, (a CYP1A2 inhibitor, 53...
2018: Journal of Toxicological Sciences
Chakradhari Inampudi, Paulino Alvarez, Rabea Asleh, Alexandros Briasoulis
Several risk factors including Ischemic heart disease, uncontrolled hypertension, high output heart failure (HF) from shunting through vascular hemodialysis access, and anemia, contribute to development of HF in patients with end-stage renal disease (ESRD). Guideline-directed medical and device therapy for Heart Failure with Reduced Ejection Fraction (HFrEF) has not been extensively studied and may have limited safety and efficacy in patients with ESRD. Maintenance of interdialytic and intradialytic euvolemia is a key component of HF management in these patients but often difficult to achieve...
January 23, 2018: Current Cardiology Reviews
Akiomi Yoshihisa
No abstract text is available yet for this article.
January 17, 2018: Circulation Journal: Official Journal of the Japanese Circulation Society
Chen Guang-Yi, Ge Li-Sha, Li Yue-Chun
The morbidity of myocarditis demonstrates an upward tendency by years, is commonly defined as the inflammation of myocytes and is caused by multiple factors. With the development of the molecular biological technique, great breakthroughs in the diagnosis and understanding of pathophysiological mechanisms of myocarditis have recently been achieved. Several questions remain unresolved, however, including standard treatment approaches to myocarditis, which remain controversial and ambiguous. Heart rate, as an independent risk factor, has been shown to be related to cardiac disease...
January 10, 2018: Current Pharmaceutical Design
Esther Kuipers, Michel Wensing, Peter A G M De Smet, Martina Teichert
RATIONALE, AIMS, AND OBJECTIVES: Despite recommendations in prevailing guidelines to avoid the use of non-selective (NS) β-blockers in patients with asthma or COPD, on average, 10 patients per community pharmacy receive NS β-blockers monthly. The aim of our study was to identify the reasons of prescribers and pharmacists to treat asthma and COPD patients with NS β-blockers. METHODS: Fifty-three community pharmacists in the Netherlands selected patients with actual concurrent use of inhalation medication and NS β-blockers...
January 10, 2018: Journal of Evaluation in Clinical Practice
Bing Huang, Youxing Li, Deqin Cheng, Guanhong He, Xing Liu, Lan Ma
Extinction learning of cocaine-associated contextual cues can help prevent cocaine addicts from relapsing. Pharmacological manipulation of β-adrenergic receptor (β-AR) during extinction learning is being developed as a potential strategy to treat drug addiction. We demonstrated that the extinction learning of cocaine-associated memory was mediated by β-arrestin2-biased but not heterotrimeric guanine nucleotide-binding protein (G protein)-dependent β-adrenergic signaling. We found that administration of the nonbiased β-AR antagonist propranolol, but not the G protein-biased β-AR antagonist carvedilol, blocked extinction learning of cocaine-conditioned place preference and the associated ERK activation in the infralimbic prefrontal cortex...
January 9, 2018: Science Signaling
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