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https://www.readbyqxmd.com/read/29159953/relationship-between-heart-failure-concurrent-chronic-obstructive-pulmonary-disease-and-beta-blocker-use-a-danish-nationwide-cohort-study
#1
Maurizio Sessa, Annamaria Mascolo, Rikke Nørmark Mortensen, Mikkel Porsborg Andersen, Giuseppe Massimo Claudio Rosano, Annalisa Capuano, Francesco Rossi, Gunnar Gislason, Henrik Enghusen-Poulsen, Christian Torp-Pedersen
AIMS: To compare the hazard of all-cause, chronic obstructive pulmonary disease (COPD) and heart failure (HF) hospitalization in carvedilol vs. metoprolol/bisoprolol/nebivolol users with COPD and concurrent HF from 2009 to 2012, and to evaluate the use and persistence in treatment of these β-blockers, their impact on the risk of COPD-related hospitalization, and the factors important for their selection. METHODS AND RESULTS: Cox and logistic regression were used for both unadjusted and adjusted analyses...
November 20, 2017: European Journal of Heart Failure
https://www.readbyqxmd.com/read/29154422/beta-blocker-dose-and-markers-of-sympathetic-activation-in-heart-failure-patients-interrelationships-and-prognostic-significance
#2
Alain Cohen-Solal, Arnold F Jacobson, Ileana L Piña
AIMS: Extent of cardiac sympathetic activation can be estimated from physiological parameters, blood biomarkers, and imaging findings. This study examined the prognostic value of three markers of sympathetic activity and their relationship to beta blocker dose in heart failure patients. METHODS AND RESULTS: A post hoc analysis of 858 heart failure subjects in the ADMIRE-HF trial was performed. Variables related to sympathetic activity were plasma norepinephrine, baseline heart rate, the heart to mediastinum (H/M) ratio of (123) I-mIBG uptake, and beta blocker dose...
November 2017: ESC Heart Failure
https://www.readbyqxmd.com/read/29151494/amiodarone-induced-hyponatremia-masked-by-tolvaptan-in-a-patient-with-an-implantable-left-ventricular-assist-device
#3
Makiko Nakamura, Osahiko Sunagawa, Tadao Kugai, Koichiro Kinugawa
A 43-year-old man was referred to our hospital in June 2014 because of severe heart failure. He was diagnosed with familial dilated cardiomyopathy and was administered oral tolvaptan and amiodarone for atrial and ventricular tachycardia. Since up-titration of carvedilol had failed and he was dependent on dobutamine, a left ventricular assist device (LVAD) was implanted. Tolvaptan and furosemide were both discontinued after LVAD implantation and he was discharged from the hospital. Thirteen months later, he was hospitalized for lethargy and hyponatremia of 108 mEq/L, with an antidiuretic hormone level of 2...
November 17, 2017: International Heart Journal
https://www.readbyqxmd.com/read/29146614/heart-rate-reduction-improves-biventricular-function-and-interactions-in-experimental-pulmonary-hypertension
#4
Olga Gomez, Kenichi Okumura, Osami Honjo, Mei Sun, Ryo Ishii, Bart Bijens, Mark K Friedberg
OBJECTIVES: To investigate mechanisms of heart rate (HR) reduction on biventricular function and interactions in experimental pulmonary arterial hypertension (PAH). METHODS: We compared cardiac-cycle mechanics and interventricular interactions in 15 sham, 8 monocrotaline-PAH, 9 PAH+carvedilol and 8 PAH+ivabradine rats. We used echocardiography to assess biventricular function, timing of cardiac- cycle events and septal position in PAH rats; and related HR reduction effect on biventricular function measured by echocardiography and conductance catheter...
November 16, 2017: American Journal of Physiology. Heart and Circulatory Physiology
https://www.readbyqxmd.com/read/29126082/artifactual-degradation-of-secondary-amine-containing-drugs-during-accelerated-stability-testing-when-saturated-sodium-nitrite-solutions-are-used-for-humidity-control
#5
Gregory W Sluggett, Todd Zelesky, Evan M Hetrick, Yelizaveta Babayan, Steven W Baertschi
Accelerated stability studies of pharmaceutical products are commonly conducted at various combinations of temperature and relative humidity (RH). The RH of the sample environment can be controlled to set points using humidity-controlled stability chambers or via storage of the sample in a closed container in the presence of a saturated aqueous salt solution. Herein we report an unexpected N-nitrosation reaction that occurs upon storage of carvedilol- or propranolol-excipient blends in a stability chamber in the presence of saturated sodium nitrite (NaNO2) solution to control relative humidity (∼60% RH)...
October 29, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/29122578/a-carvedilol-responsive-microrna-mir-125b-5p-protects-the-heart-from-acute-myocardial-infarction-by-repressing-pro-apoptotic-bak1-and-klf13-in-cardiomyocytes
#6
Ahmed S Bayoumi, Kyoung-Mi Park, Yongchao Wang, Jian-Peng Teoh, Tatsuya Aonuma, Yaoliang Tang, Huabo Su, Neal L Weintraub, Il-Man Kim
BACKGROUND: Cardiac injury is accompanied by dynamic changes in the expression of microRNAs (miRs), small non-coding RNAs that post-transcriptionally regulate target genes. MiR-125b-5p is downregulated in patients with end-stage dilated and ischemic cardiomyopathy, and has been proposed as a biomarker of heart failure. We previously reported that the β-blocker carvedilol promotes cardioprotection via β-arrestin-biased agonism of β1-adrenergic receptor while stimulating miR-125b-5p processing in the mouse heart...
November 7, 2017: Journal of Molecular and Cellular Cardiology
https://www.readbyqxmd.com/read/29115423/apoptosis-in-human-liver-carcinoma-caused-by-gold-nanoparticles-in-combination-with-carvedilol-is-mediated-via-modulation-of-mapk-akt-mtor-pathway-and-egfr-faad-proteins
#7
Raimundo F De Araújo, Jonas B Pessoa, Luis J Cruz, Alan B Chan, Emílio De Castro Miguel, Rômulo S Cavalcante, Gerly Anne C Brito, Heloiza Fernada O Silva, Luiz H S Gasparotto, Paulo M M Guedes, Aurigena A Araújo
In cancers, apoptosis signaling pathways and cell survival and growth pathways responsible for resistance to conventional treatments, such as Pi3K/Akt/mTOR and mitogen-activated protein kinase (MAPK) become dysregulated. Recently, alternative treatments to promote tumor cell death have become important. The present study reports on the antitumor and cytoprotective action of gold nanoparticles (GNPs) and carvedilol in combination and in isolated application. Apoptosis was analyzed by FITC/propidium iodide staining flow cytometry; caspase-3, caspase-8, Bcl-2 and MAPK/ERK activity by immunofluorescence microscopy; gene expression of proteins related to cell death as Akt, mTOR, EGFR, MDR1, survivin, FADD and Apaf, by the real-time PCR; and western blot analysis for MAPK/ERK, Akt and mTOR...
October 27, 2017: International Journal of Oncology
https://www.readbyqxmd.com/read/29064029/the-portal-hypertension-syndrome-etiology-classification-relevance-and-animal-models
#8
REVIEW
Jaime Bosch, Yasuko Iwakiri
BACKGROUND: Portal hypertension is a key complication of portal hypertension, which is responsible for the development of varices, ascites, bleeding, and hepatic encephalopathy, which, in turn, cause a high mortality and requirement for liver transplantation. AIM: This review deals with the present day state-of-the-art preventative treatments of portal hypertension in cirrhosis according to disease stage. Two main disease stages are considered, compensated and decompensated cirrhosis, the first having good prognosis and being mostly asymptomatic, and the second being heralded by the appearance of bleeding or non-bleeding complications of portal hypertension...
October 24, 2017: Hepatology International
https://www.readbyqxmd.com/read/29058913/drug-excipient-interactions-in-the-solid-state-the-role-of-different-stress-factors
#9
Corinna Gressl, Michael Brunsteiner, Adrian Davis, Margaret Landis, Klimentina Pencheva, Garry Scrivens, Gregory W Sluggett, Geoffrey P F Wood, Heidrun Gruber-Woelfler, Johannes G Khinast, Amrit Paudel
Understanding properties and mechanisms that govern drug degradation in the solid state is of high importance to ensure drug stability and safety of solid dosage forms. In this study, we attempt to understand drug-excipient interactions in the solid state using both theoretical and experimental approaches. The model active pharmaceutical ingredients (APIs) under study are carvedilol (CAR) and codeine phosphate (COP), which are known to undergo esterification with citric acid (CA) in the solid state. Starting from the crystal structures of two different polymorphs of each compound, we calculated the exposure and accessibility of reactive hydroxyl groups for a number of relevant crystal surfaces, as well as descriptors that could be associated with surface stabilities using molecular simulations...
November 2, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/29026706/development-of-novel-drug-eluting-stents-for-acute-myocardial-infarction
#10
REVIEW
Doo Sun Sim, Myung Ho Jeong
Delayed arterial healing at culprit sites after drug-eluting stent (DES) placement for acute myocardial infarction (AMI) is associated with increased risk of late stent thrombosis. The Korea Acute Myocardial Infarction Registry was established in commemoration of the 50(th) anniversary of Korea Circulation Society. Between November 2005 and December 2016, more than 62,000 patients were registered from 50 primary percutaneous coronary intervention (PCI) centers in Korea. DES in AMI may be safe and effective, however, there is concern about increased stent thrombosis after DES implantation in AMI patients, requiring longer-term dual anti-platelet therapy to reduce the risk of late stent thrombosis...
September 2017: Chonnam Medical Journal
https://www.readbyqxmd.com/read/29025008/cardiopulmonary-interactions-with-beta-blockers-and-inhaled-therapy-in-copd
#11
S Jabbal, W Anderson, P Short, A Morrison, A Manoharan, B J Lipworth
Background: Beta-blockers remain underused in patients with chronic obstructive pulmonary disease (COPD) and cardiovascular disease. Aim: We compared how different inhaled therapies affect tolerability of bisoprolol and carvedilol in moderate to severe COPD. Design: A randomized, open label, cross-over study. Methods: We compared the cardiopulmonary interactions of bisoprolol 5 mg qd or carvedilol 12.5 mg bid for 6 weeks in conjunction with: (i) triple: inhaled corticosteroid/long acting beta-agonist/long acting muscarinic antagonist (ICS + LABA + LAMA), (ii) dual: ICS + LABA and (iii) ICS alone...
July 24, 2017: QJM: Monthly Journal of the Association of Physicians
https://www.readbyqxmd.com/read/29016706/microrna-532-protects-the-heart-in-acute-myocardial-infarction-and-represses-prss23-a-positive-regulator-of-endothelial-to-mesenchymal-transition
#12
Ahmed S Bayoumi, Jian-Peng Teoh, Tatsuya Aonuma, Zhize Yuan, Xiaofen Ruan, Yaoliang Tang, Huabo Su, Neal L Weintraub, Il-Man Kim
Aims: Acute myocardial infarction (MI) leads to cardiac remodelling and development of heart failure. Insufficient myocardial capillary density after MI is considered a critical determinant of this process. MicroRNAs (miRs), negative regulators of gene expression, have emerged as important players in MI. We previously showed that miR-532-5p (miR-532) is up-regulated by the β-arrestin-biased β-adrenergic receptor antagonist (β-blocker) carvedilol, which activates protective pathways in the heart independent of G protein-mediated second messenger signalling...
November 1, 2017: Cardiovascular Research
https://www.readbyqxmd.com/read/28987539/statistical-investigation-of-the-full-concentration-range-of-fasted-and-fed-simulated-intestinal-fluid-on-the-equilibrium-solubility-of-oral-drugs
#13
Jeremy Perrier, Zhou Zhou, Claire Dunn, Ibrahim Khadra, Clive G Wilson, Gavin Halbert
Upon oral administration the solubility of a drug in intestinal fluid is a key property influencing bioavailability. It is also recognised that simple aqueous solubility does not reflect intestinal solubility and to optimise in vitro investigations simulated intestinal media systems have been developed. Simulated intestinal media which can mimic either the fasted or fed state consists of multiple components each of which either singly or in combination may influence drug solubility, a property that can be investigated by a statistical design of experiment technique...
October 5, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28986196/effect-of-composition-of-simulated-intestinal-media-on-the-solubility-of-poorly-soluble-compounds-investigated-by-design-of-experiments
#14
Cecilie Maria Madsen, Kung-I Feng, Andrew Leithead, Nicole Canfield, Søren Astrup Jørgensen, Anette Müllertz, Thomas Rades
The composition of the human intestinal fluids varies both intra- and inter-individually. This will influence the solubility of orally administered drug compounds, and hence, the absorption and efficacy of compounds displaying solubility limited absorption. The purpose of this study was to assess the influence of simulated intestinal fluid (SIF) composition on the solubility of poorly soluble compounds. Using a Design of Experiments (DoE) approach, a set of 24 SIF was defined within the known compositions of human fasted state intestinal fluid...
October 3, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28977354/thin-layer-chromatographic-resolution-of-some-%C3%AE-adrenolytics-and-a-%C3%AE-2-agonist-using-bovine-serum-albumin-as-chiral-additive-in-stationary-phase
#15
Poonam Malik, Ravi Bhushan
Direct enantiomeric resolution of commonly used five racemic β-adrenolytics, namely, bisoprolol, atenolol, propranolol, salbutamol and carvedilol has been achieved by thin layer chromatography using bovine serum albumin (BSA) as chiral additive in stationary phase. Successful resolution of the enantiomers of all racemic β-adrenolytics was achieved by use of different composition of simple organic solvents having no buffer or inorganic ions. The effect of variation in pH, temperature, amount of BSA as the additive, and composition of mobile phase on resolution was systematically studied...
September 15, 2017: Journal of Chromatographic Science
https://www.readbyqxmd.com/read/28967043/jet-dispensing-of-multi-layered-films-for-the-co-delivery-of-three-antihypertensive-agents
#16
Nicolaos Scoutaris, Maria Malamatari, Adrien Letellier, Dennis Douroumis
Three-layer thin films comprising of two polymers as substrate (ethyl cellulose and, copovidone K28) and three antihypertensive agents (hydrochlorothiazide, amiloride HCl, and carvedilol) were printed using jet dispensing technology. Two film formulations with different ethyl cellulose to copovidone K28 ratio (i.e., 90/10 and 50/50 w/w) were prepared using a three-course dispensing. The films were characterized regarding surface morphology, solid-state properties, polymer-drug interactions, drug distribution in each layer, and in vitro drug release...
October 2, 2017: Drug Delivery and Translational Research
https://www.readbyqxmd.com/read/28942006/effect-of-dronedarone-on-the-pharmacokinetics-of-carvedilol-following-oral-administration-to-rats
#17
Min-Soo Kim, In-Hwan Baek
Dronedarone is a CYP2D6 inhibitor; therefore, it is prudent to exercise caution when concurrently administering CYP2D6-metabolized β-blockers because of a lack of published data on potential drug interactions. The aim of this study was to investigate the effect of dronedarone on the pharmacokinetics of orally administered carvedilol in rats. Twenty male Sprague-Dawley rats were randomly divided into two groups and 10mg/kg carvedilol was administered to the rat with or without dronedarone pretreatment in a parallel design...
September 20, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28936473/carvedilol-for-the-treatment-of-red-scrotum-syndrome
#18
Ribal Merhi, Nakhle Ayoub, Marc Mrad
No abstract text is available yet for this article.
September 2017: JAAD Case Reports
https://www.readbyqxmd.com/read/28912118/topically-applied-carvedilol-attenuates-solar-ultraviolet-radiation-induced-skin-carcinogenesis
#19
Kevin M Huang, Sherry Liang, Steven Yeung, Etuajie Oiyemhonlan, Kristan H Cleveland, Cyrus Parsa, Robert Orlando, Frank L Meyskens, Bradley T Andresen, Ying Huang
In previous studies, the β-blocker carvedilol inhibited EGF-induced epidermal cell transformation and chemical carcinogen-induced mouse skin hyperplasia. As exposure to ultraviolet (UV) radiation leads to skin cancer, the present study examined whether carvedilol can prevent UV-induced carcinogenesis. Carvedilol absorbs UV like a sunscreen; thus, to separate pharmacological from sunscreen effects, 4-hydroxycarbazole (4-OHC), which absorbs UV to the same degree as carvedilol, served as control. JB6 P(+) cells, an established epidermal model for studying tumor promotion, were used for evaluating the effect of carvedilol on UV-induced neoplastic transformation...
August 15, 2017: Cancer Prevention Research
https://www.readbyqxmd.com/read/28911302/what-is-the-real-efficacy-of-beta-blockers-for-the-treatment-of-essential-hypertension
#20
Christian Höcht, Facundo M Bertera, Julieta S Del Mauro, Yanina Santander Plantamura, Carlos A Taira, Ariel H Polizio
OBJECTIVE: This review covers the pharmacokinetics and pharmacodynamic of β-blockers, the rationale for their use, some recent controversies in its use for managing hypertension, as well as, the beneficial properties of the third-generation β-blockers beyond hypertension. BACKGROUND: The efficacy and safety of -blockers in the treatment of hypertension and other cardiovascular diseases have been established during more than 50 years of clinical experience. Recent updates of clinical guidelines have downgraded the use of -blockers for the treatment of uncomplicated hypertension to second and third line therapy...
June 7, 2017: Current Pharmaceutical Design
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