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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
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)...
October 25, 2016: Chemistry: a European Journal
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
Luke C Zona, Gregory G Grecco, Jon E Sprague
The use of the synthetic cathinones ("bath salts"), methylone and mephedrone, has been associated with the development of life-threatening hyperthermia. To date, no direct pharmacological intervention to mitigate the hyperthermia induced by synthetic cathinones has been identified. Here, we investigated the effects of the non-selective α1 and β adrenergic receptor antagonist carvedilol (5mg/kg ip) on established hyperthermia mediated by methylone and mephedrone (30mg/kg sc) in Sprague-Dawley rats. Methylone and mephedrone induced a hyperthermic response that peaked 60minutes post treatment...
October 20, 2016: Toxicology Letters
Naokata Sumitomo
Catecholaminergic polymorphic ventricular tachycardia (CPVT) is induced by emotions or exercise in patients without organic heart disease and may be polymorphic or bidirectional in nature. The prognosis of CPVT is not good, and therefore prevention of sudden death is of utmost importance. Genetic variants of CPVT include RyR2, CASQ2, CALM2, TRD, and possibly KCNJ2 and ANK2 gene mutations. Hypotheses that suggest the causes of CPVT include weakened binding of FKBP12.6 and RyR2, a store overload-induced Ca(2+) release (SOICR), unzipping of intramolecular domain interactions in RyR2, and molecular and functional abnormalities caused by mutations in the CASQ2 gene...
October 2016: Journal of Arrhythmia
Saleh Ayashi, Ahmad Reza Assareh, Mohammad Taha Jalali, Samaneh Olapour, Hamid Yaghooti
OBJECTIVE: Carvedilol is a nonselective third generation β-blocker that does not display the negative effects of traditional β-blockers. Regarding the antioxidant, anti-inflammatory and distinct metabolic properties of carvedilol which are similar to that of high-density lipoprotein (HDL) and paraoxonase 1 (PON1), the present study intends to investigate the effects of carvedilol treatment on malondialdehyde (MDA) and soluble lectin-like ox-low-density lipoprotein (LDL) receptor (sLOX-1) as markers of oxidative stress in association to lipid profiles, apolipoproteins (apo), and PON1 activity in hypertensive patients...
July 2016: Indian Journal of Pharmacology
Dong-Seok Yim
In the early phase of clinical development of antihypertensive drugs, quantitative modeling to predict their dose-concentration-response relationship is important to plan future clinical development and finding optimal dosage regimen at marketing approval. Two cases of concentration-response models of antihypertensive are presented here.Case 1: Carvedilol is a α1- and nonselective β- adrenergic receptor antagonist currently used for the management of mild-to-moderate essential hypertension and congestive heart failure...
September 2016: Journal of Hypertension
Hae-Young Lee, Chan-Soon Park, Sang-Hoon Na, Kyung-Jin Kim, Chan Joo Lee, Sungha Park
A 47-year-old woman was admitted via emergency department due to dyspnea NYHA Fc II-III aggravated for 2 months after upper respiratory infection. Her height and body weight were 161 cm / 67 kg. Initial vital signs were 110/70 mmHg - 112 BPM - 24/min - 36.5°C. Chest PA showed cardiomegaly and pulmonary congestion (Figure 1). B-natriuretic peptide level was markedly increased (2002 pg/mL, normal range ≤ 100 pg/mL). The echocardiographic examination showed severely dilated LV cavity (61/72 mm) and severe LV systolic dysfunction (EF 28%) with normal left ventricular wall thickness (9/11 mm) (Figure 2)...
September 2016: Journal of Hypertension
Chan Joo Lee, Yeongmin Woo, Byeong-Keuk Kim, Kyung Bong Yoon, Hae-Young Lee, Sungha Park
A 30-year-old woman was referred to our hospital due to high blood pressure, dizziness, headache and blurred vision. She had past history of preeclampsia and gestational hypertension 4 years ago but she had not taken antihypertensive medication in spite of remained hypertension after delivery. She was hospitalized for fever due to urinary tract infection and severe hypertension which was above 210/140 mmHg. Despite maximal medical treatment with telmisartan 80 mg, nifedipine 120 mg, carvedilol 50 mg, doxazocin 8 mg, chlorthalidone 50 mg, spironolactone 50 mg#2, isosorbide dinitrate 80 mg and intermittent intravenous administration of nicardipine and labetalol, her systolic blood pressure remained above 160 mmHg and repeatedly measured above 200 mmHg...
September 2016: Journal of Hypertension
Meghan MacKenzie, Richard Hall
PURPOSE: Knowledge of how alterations in pharmacogenomics and pharmacogenetics may affect drug therapy in the intensive care unit (ICU) has received little study. We review the clinically relevant application of pharmacogenetics and pharmacogenomics to drugs and conditions encountered in the ICU. SOURCE: We selected relevant literature to illustrate the important concepts contained within. PRINCIPAL FINDINGS: Two main approaches have been used to identify genetic abnormalities - the candidate gene approach and the genome-wide approach...
October 17, 2016: Canadian Journal of Anaesthesia, Journal Canadien D'anesthésie
Vijendra Kirnake, Anil Arora, Varun Gupta, Praveen Sharma, Vikas Singla, Naresh Bansal, Mohan Goyal, Romesh Chawlani, Ashish Kumar
BACKGROUND: Non-selective beta-blockers (NSBBs), e.g. propranolol, are recommended for prophylaxis of variceal bleeding in cirrhosis. Carvedilol, a newer NSBB with additional anti-α1-adrenergic activity, is superior to propranolol in reducing portal pressure. Repeated HVPG measurements are required to identify responders to NSBB. We aimed to determine whether a single-time HVPG measurement, using acute-hemodynamic-response-testing, is sufficient to predict long-term response to carvedilol, and whether these responders have better clinical outcome...
September 2016: Journal of Clinical and Experimental Hepatology
Mohamed Balaha, Samah Kandeel, Waleed Barakat
Carvedilol is an anti-oxidant non-selective β-blocker used for reduction of portal blood pressure, prophylaxis of esophageal varices development and bleeding in chronic liver diseases. Recently, it exhibited potent anti-inflammatory, anti-fibrotic, anti-proliferative and anti-carcinogenic effects. In the present study, we evaluated the possible suppressive effect of carvedilol on circulating and hepatic IL-6 levels responsible for hepatocarcinogenesis in a rat model of hepatic cirrhosis. Besides, its effect on hepatic STAT-3 levels, function tests, oxidative stress markers, and hydroxyproline content, hepatic tissue histopathological changes and immunohistochemical expression of E & N-cadherin...
October 13, 2016: Toxicology and Applied Pharmacology
Zhigang Li, Baoyi Liu, Benjie Wang, Yupeng Liu, Yao Zhang, Fengde Tian, Borui Li, Dewei Zhao
Collagen type Ⅱ (col Ⅱ) and aggrecan, the main components of the extracellular matrix (ECM) in human joint cartilage, have been reported to be reduced by chronic production of inflammatory cytokine interleukin (IL)-1β in arthritic joints. Carvedilol, a licensed medicine, has been used for treatment of hypertension, congestive heart failure and coronary disease in clinics. In this study, we investigated the effects of Carvedilol on the expression of col Ⅱ and aggrecan. Our results demonstrate that treatment with Carvedilol didn't change the expression of aggrecan or col Ⅱ at mRNA levels in SW1353 chondrocytes...
October 13, 2016: Biochemical and Biophysical Research Communications
Darjan Košir, Franc Vrečer
CONTEXT: The flow and compaction properties of a compaction mixture or powder and the drug-release profile of final tablets are important critical quality attributes (CQAs) that have an impact on the overall performance of hydrophilic matrix tablets. The selection of granulation method can importantly affect these CQAs. OBJECTIVE: This study investigates various agglomeration methods of sustained-release formulation using HPMC K4M as a release polymer with various wet- and dry-granulation techniques...
October 14, 2016: Drug Development and Industrial Pharmacy
Zhichao Xiao, Wenting Guo, Bo Sun, Donald J Hunt, Jinhong Wei, Yingjie Liu, Yundi Wang, Ruiwu Wang, Peter P Jones, Thomas G Back, S R Wayne Chen
Recent three-dimensional structural studies reveal that the Central domain of ryanodine receptor (RyR) serves as a transducer that converts long-range conformational changes into the gating of the channel pore. Interestingly, the Central domain encompasses one of the mutation hotspots (corresponding to amino acid residues 3778-4201) that contains a number of cardiac RyR (RyR2) mutations associated with catecholaminergic polymorphic ventricular tachycardia (CPVT) and atrial fibrillation (AF). However, the functional consequences of these Central domain RyR2 mutations are not well understood...
October 12, 2016: Journal of Biological Chemistry
Kyyak Hryhoriy
INTRODUCTION: type 2 diabetes mellitus is one of the most important medical and social problems in the world. Patients with diabetes are prone to coronary artery disease, in particular acute coronary syndrome, with atypical clinical signs and susceptibility to tachycardia. Elevated heart rate is an important factor of premature mortality in all patients with acute coronary syndrome. The aim of the investigation was to reveal the heart rate peculiarities in unstable angina and non-ST elevation myocardial infarction patients suffering from diabetes mellitus type 2 for more effective treatment of these patients...
2016: Wiadomości Lekarskie: Organ Polskiego Towarzystwa Lekarskiego
Mattias Mandorfer, Thomas Reiberger
To date, non-selective beta blockers (NSBBs) are a cornerstone in the treatment of portal hypertension. During the last years, our understanding of the potential benefits of early initiation of NSBB treatment, their effects beyond the prevention of variceal bleeding (i.e., their non-hemodyamic effects), as well as potential detrimental effects in patients with advanced disease has continuously evolved. In addition, we have learned that not all NSBBs are equal. Due to its additional anti-α1-adrenergic activity, carvedilol has been shown to be more potent in decreasing portal pressure, but might lead to more pronounced decreases in systemic arterial pressure, when compared to conventional NSBBs...
September 27, 2016: Digestive and Liver Disease
Saro H Armenian, Melissa M Hudson, Ming Hui Chen, Steven D Colan, Lanie Lindenfeld, George Mills, Aida Siyahian, Sarah Gelehrter, Ha Dang, Wendy Hein, Daniel M Green, Leslie L Robison, F Lennie Wong, Pamela S Douglas, Smita Bhatia
BACKGROUND: Anthracyclines are widely used in the treatment of childhood cancer. One of the well-recognized side-effects of anthracycline therapy is dose-dependent cardiomyopathy that may progress to heart failure (HF) years after completion of cancer-directed therapy. This study will evaluate the efficacy of low-dose beta-blocker (carvedilol) for HF risk reduction in childhood cancer survivors at highest risk for HF. The proposed intervention has the potential to significantly reduce chronic cardiac injury via interruption of neurohormonal systems responsible for left ventricular (LV) remodeling, resulting in improved cardiac function and decreased risk of HF...
October 4, 2016: BMC Cardiovascular Disorders
Ahmed Atwa, Rehab Hegazy, Nermeen Shaffie, Neamat Yassin, Sanaa Kenawy
BACKGROUND: Rhabdomyolysis (RM)-induced acute renal failure (ARF) accounts for about 10-40% of all cases of ARF. AIM: The present study investigated the possible protective effect of two nitric oxides (NO)-releasing third generation β-blockers, carvedilol (Carv) and nebivolol (Nebi), against RM-mimicking glycerol (Gly)-induced ARF in rats. MATERIAL AND METHODS: After 24 h dehydration, rats received a single dose of 50% Gly (8 ml/kg, im). They were treated with vehicle, Carv (2...
September 15, 2016: Open Access Macedonian Journal of Medical Sciences
Catherine Girouard, Jean-Pierre Grégoire, Paul Poirier, Jocelyne Moisan
PURPOSE: β-Blockers (bisoprolol, carvedilol, and metoprolol) are the cornerstone of heart failure (HF) management. The incidence rate of β-blocker initiation and discontinuation and their associated factors among seniors with a first HF diagnosis were assessed. METHODS: A population-based inception cohort study that included all individuals aged ≥65 years with a first HF diagnosis in Quebec was conducted. β-Blockers initiation among 91,131 patients who were not using β-blockers at the time of HF diagnosis and discontinuation among those who initiated a β-blocker after HF diagnosis were assessed...
2016: Patient Preference and Adherence
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