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https://www.readbyqxmd.com/read/27920825/evaluation-of-cardioprotective-effect-of-aqueous-extract-of-allium-cepa-linn-bulb-on-isoprenaline-induced-myocardial-injury-in-wistar-albino-rats
#1
Geeta B Kharadi, Kaksha J Patel, Bhargav M Purohit, Seema N Baxi, C B Tripathi
To investigate the cardioprotective potential of the aqueous extract of Allium cepa Linn. bulb in isoprenaline-induced myocardial injury in Wistar albino rats. In vitro total phenolic, total flavonoid content and 2, 2'-diphenyl-1-picrylhydrazyl hydrate radical scavenging activity was measured. Isoprenaline-induced myocardial injury model was used to evaluate in vivo effect of aqueous extract of A. cepa in Wistar albino rats. Seventy two rats were randomly divided in 6 groups. Rats were treated with A. cepa 400 mg/kg and 800 mg/kg doses for 30 days and myocardial injury was produced by subcutaneous injection of isoprenaline (ISO) 85 mg/kg on day 28 and 29...
October 2016: Research in Pharmaceutical Sciences
https://www.readbyqxmd.com/read/27899231/carvedilol-exacerbate-gentamicin-induced-kidney-mitochondrial-alterations-in-adult-rat
#2
Luís Félix, M M Oliveira, Romeu Videira, Elisabete Maciel, Nuno D Alves, Fernando M Nunes, Anabela Alves, José M Almeida, M Rosário M Domingues, Francisco P Peixoto
Gentamicin is an aminoglycoside antibiotic widely used to treat many types of bacterial infections. Although its properties, his clinical use is limited due to the occurrence of nephrotoxicity, which has been related to mitochondrial dysfunction. Carvedilol, an antihypertensive drug with strong antioxidant properties, has been tested in order to prevent gentamicin nephrotoxicity. This study aimed to test this hypothesis using a rat model of gentamicin-induced nephrotoxicity. Animals were treated subcutaneously with DMSO (control) (0...
November 26, 2016: Experimental and Toxicologic Pathology: Official Journal of the Gesellschaft Für Toxikologische Pathologie
https://www.readbyqxmd.com/read/27889753/renal-denervation-attenuates-multi-organ-fibrosis-and-improves-vascular-remodeling-in-rats-with-transverse-aortic-constriction-induced-cardiomyopathy
#3
Kai Wang, Dasheng Lu, Bin Zhang, Shengchan Wang, Qian Liu, Qi Zhang, Jie Geng, Qijun Shan
BACKGROUND/AIMS: To investigate the effects of renal denervation (RDN) on multi-organ fibrosis and vascular remodeling in cardiomyopathy. METHODS: Thirty-six male Sprague-Dawley rats underwent transverse aortic constriction (TAC). Five weeks later, 28 surviving TAC rats were randomly assigned to three groups: (1) RDN, (2) Sham, (3) Carvedilol. Six male Sham TAC rats served as the Control. Ten weeks after TAC, samples were collected. RESULTS: TAC rats showed an increased diastolic interventricular septal thickness at week 5...
November 25, 2016: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/27886776/synthesis-and-performance-of-chiral-ferrocene-modified-silica-gel-for-mixed-mode-chromatography
#4
Lijun Qiao, Xiaohua Zhou, Xue Li, Wenrui Du, Ajuan Yu, Shusheng Zhang, Yangjie Wu
A brush-type chiral stationary phase, N-ferrocenyl benzoyl-(1S, 2R)-1, 2-diphenyl ethanol-bonded on the silica gel (NFcBEs) for high performance liquid chromatography (HPLC), was prepared using γ-glycidoxypropyltrimethoxysilane as coupling reagent. The structure of this novel material was characterized by infrared spectroscopy, elemental analysis and thermogravimetric analysis. Mechanism involved in the chromatographic separation is the multi-interaction including hydrophobic, π-π, hydrogen-bonding, π-charge transfer, dipole-dipole and acid-base equilibrium interactions...
January 15, 2017: Talanta
https://www.readbyqxmd.com/read/27879163/a-study-of-critical-functionality-related-characteristics-of-hpmc-for-sustained-release-tablets
#5
Darjan Košir, Tadej Ojsteršek, Saša Baumgartner, Franc Vrečer
The drug release profile from hydrophilic matrix tablets can be crucially affected by the variability of physicochemical properties of the controlled release agent. This study investigates and seeks to understand the functionality-related characteristics (FRCs) of hydroxypropyl methylcellulose (HPMC) type 2208, K4M grade, that influence the release rate of the model drug carvedilol from hydrophilic matrix tablets during the entire dissolution profile. The following FRCs were examined: particle size distribution, degree of substitution, and viscosity...
November 23, 2016: Pharmaceutical Development and Technology
https://www.readbyqxmd.com/read/27869375/aktueller-stand-der-systemischen-rosazea-therapie
#6
M Schaller, H Schöfer, B Homey, U Gieler, P Lehmann, T A Luger, T Ruzicka, M Steinhoff
Basierend auf den Daten zahlreicher Studien sind orale Tetracycline - und hier insbesondere Doxycyclin als Tetracyclin der zweiten Generation - die Grundpfeiler der systemischen Rosazea-Therapie. Bisher ist dafür jedoch nur Doxycyclin 40 mg in antientzündlicher Dosierung mit veränderter Wirkstofffreisetzung zugelassen. Seit Einführung der Therapie mit Doxycyclin einmal täglich in nicht antibiotischer Dosierung wird die orale Therapie häufiger als Erstbehandlung bei mittelschwerer bis schwerer papulopustulöser Rosazea verschrieben...
December 2016: Journal der Deutschen Dermatologischen Gesellschaft, Journal of the German Society of Dermatology: JDDG
https://www.readbyqxmd.com/read/27869374/state-of-the-art-systemic-rosacea-management
#7
M Schaller, H Schöfer, B Homey, U Gieler, P Lehmann, T A Luger, T Ruzicka, M Steinhoff
Based on numerous trials, oral tetracyclines and most commonly their second-generation derivative doxycycline have become the main pillar in systemic rosacea treatment. However, the only preparation that has been approved so far in this setting is 40 mg doxycycline in an anti-inflammatory dosage and with a modified release formulation. With the introduction of this once-daily, non-antibiotic dosing of doxycycline, oral therapy is more commonly prescribed as first-line treatment in moderate to severe papulopustular rosacea...
December 2016: Journal der Deutschen Dermatologischen Gesellschaft, Journal of the German Society of Dermatology: JDDG
https://www.readbyqxmd.com/read/27859924/older-adults-with-heart-failure-treated-with-carvedilol-bisoprolol-or-metoprolol-tartrate-risk-of-mortality
#8
Sylvie Perreault, Simon de Denus, Michel White, Brian White-Guay, Michel Bouvier, Marc Dorais, Marie-Pierre Dubé, Jean-Lucien Rouleau, Jean-Claude Tardif, Sarah Jenna, Benjamin Haibe-Kains, Richard Leduc, Denis Deblois
PURPOSE: The long-term use of β-blockers has been shown to improve clinical outcomes among patients with heart failure (HF). However, a lack of data persists in assessing whether carvedilol or bisoprolol are superior to metoprolol tartrate in clinical practice. We endeavored to compare the effectiveness of β-blockers among older adults following a primary hospital admission for HF. METHODS: We conducted a cohort study using Quebec administrative databases to identify patients who were using β-blockers, carvedilol, bisoprolol, or metoprolol tartrate after the diagnosis of HF...
November 16, 2016: Pharmacoepidemiology and Drug Safety
https://www.readbyqxmd.com/read/27836712/application-of-substrate-depletion-assay-to-evaluation-of-cyp-isoforms-responsible-for-stereoselective-metabolism-of-carvedilol
#9
Masahiro Iwaki, Toshiro Niwa, Saya Bandoh, Megumi Itoh, Hitomi Hirose, Atsushi Kawase, Hiroshi Komura
To evaluate the relative contribution of cytochrome P450 (CYP) isoforms responsible for carvedilol (CAR) oxidation, enantioselective metabolism of CAR was investigated in human liver microsomes (HLMs) and recombinant human CYPs by using the substrate depletion assay. CYP2D6 exhibited the highest contribution to the metabolism of R-CAR, followed by CYP3A4, CYP1A2, and CYP2C9, whereas the metabolism of the S-enantiomer was mainly mediated by CYP1A2, followed by CYP2D6 and CYP3A4. In HLMs, metabolism of R- and S-CAR was markedly inhibited by quinidine; R-CAR metabolism (57-61% decrease) was more inhibited than S-CAR metabolism (37-43% decrease), and furafylline and ketoconazole almost equally inhibited metabolism of both enantiomers by 25-32% and 30-50%, respectively...
September 2, 2016: Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/27827372/functional-competence-of-a-partially-engaged-gpcr-%C3%AE-arrestin-complex
#10
Punita Kumari, Ashish Srivastava, Ramanuj Banerjee, Eshan Ghosh, Pragya Gupta, Ravi Ranjan, Xin Chen, Bhagyashri Gupta, Charu Gupta, Deepika Jaiman, Arun K Shukla
G Protein-coupled receptors (GPCRs) constitute the largest family of cell surface receptors and drug targets. GPCR signalling and desensitization is critically regulated by β-arrestins (βarr). GPCR-βarr interaction is biphasic where the phosphorylated carboxyl terminus of GPCRs docks to the N-domain of βarr first and then seven transmembrane core of the receptor engages with βarr. It is currently unknown whether fully engaged GPCR-βarr complex is essential for functional outcomes or partially engaged complex can also be functionally competent...
November 9, 2016: Nature Communications
https://www.readbyqxmd.com/read/27818482/high-dose-%C3%AE-blocker-therapy-triggers-additional-reverse-remodeling-in-patients-with-idiopathic-non-ischemic-cardiomyopathy
#11
Daisuke Nitta, Koichiro Kinugawa, Teruhiko Imamura, Naoko P Kato, Issei Komuro
Carvedilol has established its evidence to improve prognosis and facilitate left ventricular reverse remodeling (LVRR) in heart failure patients with reduced left ventricular ejection fraction (LVEF), and many studies have supported its dose-dependency. However, there are few studies demonstrating the effect of high dose carvedilol in Japan. We enrolled 23 patients with idiopathic non-ischemic cardiomyopathy, in whom LVEF remained 45% or less despite 20 mg/ day of carvedilol therapy for > 3 months. After high dose (40 mg/day) carvedilol therapy for > 3 months, LVEF improved (+9...
November 4, 2016: International Heart Journal
https://www.readbyqxmd.com/read/27818454/vidarabine-an-anti-herpes-virus-agent-protects-against-the-development-of-heart-failure-with-relatively-mild-side-effects-on-cardiac-function-in-a-canine-model-of-pacing-induced-dilated-cardiomyopathy
#12
Takashi Nakamura, Takayuki Fujita, Megumi Kishimura, Kenji Suita, Yuko Hidaka, Wenqian Cai, Masanari Umemura, Utako Yokoyama, Masami Uechi, Yoshihiro Ishikawa
BACKGROUND: In heart failure patients, chronic hyperactivation of sympathetic signaling is known to exacerbate cardiac dysfunction. In this study, the cardioprotective effect of vidarabine, an anti-herpes virus agent, which we identified as a cardiac adenylyl cyclase inhibitor, in dogs with pacing-induced dilated cardiomyopathy (DCM) was evaluated. In addition, the adverse effects of vidarabine on basal cardiac function was compared to those of the β-blocker, carvedilol.Methods and Results:Vidarabine and carvedilol attenuated the development of pacing-induced systolic dysfunction significantly and with equal effectiveness...
November 5, 2016: Circulation Journal: Official Journal of the Japanese Circulation Society
https://www.readbyqxmd.com/read/27815373/inhibiting-insulin-mediated-%C3%AE-2ar-activation-prevents-diabetes-associated-cardiac-dysfunction
#13
Qingtong Wang, Yongming Liu, Qin Fu, Bing Xu, Yuan Zhang, Sungjin Kim, Ruensern Tan, Federica Barbagallo, Toni M West, Ethan J Anderson, Wei Wei, E Dale Abel, Yang K Xiang
BACKGROUND: -Type-2 diabetes and obesity independently increases the risk of heart failure via incompletely understood mechanisms. We propose that hyperinsulinemia might promote adverse consequences in hearts of subjects with type-2 diabetes and obesity. METHODS: -High fat diet feeding was used to induce obesity and diabetes in wild type mice or mice lacking β 2-adrenergic receptor (β2AR) or β -arrestin2. Wild type mice fed with high fat diet were treated with β -blocker carvedilol or G-protein receptor kinase 2 (GRK2) inhibitor...
November 4, 2016: Circulation
https://www.readbyqxmd.com/read/27809882/comparative-effects-of-nebivolol-and-carvedilol-on-left-ventricular-diastolic-function-in-older-heart-failure-patients-with-preserved-ejection-fraction-study-protocol-for-a-randomized-controlled-trial
#14
Kyungil Park, Tae-Ho Park
BACKGROUND: Heart failure (HF) is a common and disabling condition in older people. Randomized clinical trials and meta-analyses have clearly demonstrated that the long-term use of β-Blockers improves the outcome of patients with HF. However, limited data are available on the treatment of older HF patients with preserved ejection fraction (EF). No study has specifically compared the relative effectiveness of carvedilol and nebivolol in treating HF in older patients with preserved EF...
November 3, 2016: Trials
https://www.readbyqxmd.com/read/27805735/carvedilol-and-antioxidant-proteins-in-a-type-i-diabetes-animal-model
#15
Cátia V Diogo, Cláudia M Deus, Magdalena Lebiedzinska-Arciszewska, Aleksandra Wojtala, Mariusz R Wieckowski, Paulo J Oliveira
BACKGROUND: Patients with diabetes are at a high risk of developing both micro- and macro-vascular disease. Hyperglycaemia seems to be the main factor in the pathogenesis of diabetic cardiomyopathy, often based on increased oxidative stress. Carvedilol, a β-adrenergic blocker has intrinsic antioxidant properties and was previously described to be effective in the protection of cardiac mitochondria against oxidative stress. The objective of this study was to evaluate the effect of Carvedilol on hyperglycaemia-induced oxidative damage and mitochondrial abnormalities in cardiac and skeletal muscle in streptozotocin-treated rats...
November 2, 2016: European Journal of Clinical Investigation
https://www.readbyqxmd.com/read/27804100/rhabdomyolysis-after-coadministration-of-atorvastatin-and-sacubitril-valsartan-entresto%C3%A2-in-a-63-year-old-woman
#16
Eve S Faber, Madhavi Gavini, Ronald Ramirez, Richard Sadovsky
A 63-year-old woman previously stable on a regimen of atorvastatin 40 mg daily, carvedilol 25 mg twice daily, digoxin 0.125 mg daily, furosemide 40 mg daily, spironolactone 25 mg daily, rivaroxaban 15 mg daily, and enalapril 20 mg twice daily for heart failure developed rhabdomyolysis 26 days after enalapril was stopped and sacubitril/valsartan (Entresto™) started. The patient received sacubitril/valsartan at 24/26 mg twice daily for heart failure; however, after 26 days she developed muscle and skin pain...
December 2016: Drug Safety—Case Reports
https://www.readbyqxmd.com/read/27792991/protective-effects-of-bisoprolol-against-myocardial-injury-and-pulmonary-dysfunction-in-patients-with-chronic-heart-failure
#17
Shigeru Toyoda, Akiko Haruyama, Shu Inami, Hirohisa Amano, Takuo Arikawa, Masashi Sakuma, Shichiro Abe, Atsushi Tanaka, Koichi Node, Teruo Inoue
OBJECTIVES: This study was designed to elucidate differences in effects of 2 beta blockers, bisoprolol and carvedilol, in patients with chronic heart failure. BACKGROUND: Although the beta blockers bisoprolol and carvedilol are commonly used in patients with chronic heart failure, differences in the efficacy and safety of these medications have not been established in this patient population. METHODS: Patients with chronic systolic heart failure, defined as ≤45% ejection fraction, who had received intensive medical therapy with the exception of beta blockers, were randomly assigned to receive either bisoprolol or carvedilol for 24weeks...
October 22, 2016: International Journal of Cardiology
https://www.readbyqxmd.com/read/27780169/the-effects-of-carvedilol-on-cardiac-function-and-the-akt-xiap-signaling-pathway-in-diabetic-cardiomyopathy-rats
#18
Wencheng Zheng, Xiaoming Shang, Chunlai Zhang, Xiang Gao, Barry Robinson, Jing Liu
OBJECTIVES: Diabetic cardiomyopathy (DCM) is characterized by cardiac dysfunction, myocardial inflammation, interstitial fibrosis and cardiomyocytes apoptosis. The present study aimed to investigate the effects of carvedilol on cardiac function and the AKT/XIAP signaling pathway in DCM rats. METHODS: Male Wistar rats were randomly divided into 3 groups: the control group, diabetic mellitus (DM) group and DM with carvedilol treatment group. DM rats were induced by streptozotocin accompanied by high energy intake...
October 26, 2016: Cardiology
https://www.readbyqxmd.com/read/27778384/synthesis-of-glycoborine-glybomine-a-and-b-the-phytoalexin-carbalexin-a-and-the-%C3%AE-adrenoreceptor-antagonists-carazolol-and-carvedilol
#19
Christian Brütting, Ronny Hesse, Anne Jäger, Olga Kataeva, Arndt W Schmidt, Hans-Joachim Knölker
We describe a regioselective synthesis of 4- or 5-substituted carbazoles by oxidative cyclisation of meta-oxygen-substituted N-phenylanilines. Using the regiodirecting effect of a pivaloyloxy group, we prepared 4-hydroxycarbazole, a precursor for the enantiospecific synthesis of the β-adrenoreceptor antagonists (-)-(S)-carazolol (5) and (-)-(S)-carvedilol (6). Regioselective palladium(II)-catalysed cyclisation of different diarylamines led to total synthesis of glycoborine (7) and the first total syntheses of the phytoalexin carbalexin A (8), glybomine A (9) and glybomine B (10)...
November 14, 2016: Chemistry: a European Journal
https://www.readbyqxmd.com/read/27777006/inhibition-of-plasma-lipid-oxidation-induced-by-peroxyl-radicals-peroxynitrite-hypochlorite-15-lipoxygenase-and-singlet-oxygen-by-clinical-drugs
#20
Mayuko Morita, Yuji Naito, Toshikazu Yoshikawa, Etsuo Niki
With increasing evidence showing the involvement of oxidative stress in the pathogenesis of various diseases, the effects of clinical drugs possessing antioxidant functions have received much attention. The unregulated oxidative modification of biological molecules leading to diseases is mediated by multiple oxidants including free radicals, peroxynitrite, hypochlorite, lipoxygenase, and singlet oxygen. The capacity of antioxidants to scavenge or quench oxidants depends on the nature of oxidants. In the present study, the antioxidant effects of several clinical drugs against plasma lipid oxidation induced by the aforementioned five kinds of oxidants were investigated from the production of lipid hydroperoxides, which have been implicated in the pathogenesis of various diseases...
October 13, 2016: Bioorganic & Medicinal Chemistry Letters
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