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https://www.readbyqxmd.com/read/28912118/topically-applied-carvedilol-attenuates-solar-ultraviolet-radiation-induced-skin-carcinogenesis
#1
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
#2
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
https://www.readbyqxmd.com/read/28894360/the-evaluation-of-%C3%AE-adrenoceptor-blocking-agents-in-patients-with-copd-and-congestive-heart-failure-a-nationwide-study
#3
Kuang-Ming Liao, Tien-Yu Lin, Yaw-Bin Huang, Chen-Chun Kuo, Chung-Yu Chen
OBJECTIVE: β-Blockers are safe and improve survival in patients with both congestive heart failure (CHF) and COPD. However, the superiority of different types of β-blockers is still unclear among patients with CHF and COPD. The association between β-blockers and CHF exacerbation as well as COPD exacerbation remains unclear. The objective of this study was to compare the outcome of different β-blockers in patients with concurrent CHF and COPD. PATIENTS AND METHODS: We used the National Health Insurance Research Database in Taiwan to conduct a retrospective cohort study...
2017: International Journal of Chronic Obstructive Pulmonary Disease
https://www.readbyqxmd.com/read/28891709/-carvedilol-in-the-everyday-interventional-cardiology-practice
#4
Attila Kónyi
The treatment of severe coronary stenoses with stent implantation is very effective nevertheless, the underlying problem of atherosclerosis remains unsolved with the implantation of a stent. Therefore, besides lifestyle changes, the adequate medication therapy is of pivotal importance. In the majority of patients scheduled for or acutely undergoing catheterisation, beta-blockers form the basis of medication therapy. Members of the group, however, show significant differences in terms of pharmacodynamics. The third-generation beta-blocker and vasodilator carvedilol possesses complex adrenerg-blocking and Ca-channel blocking effects as well...
September 2017: Orvosi Hetilap
https://www.readbyqxmd.com/read/28883225/anemia-is-associated-with-blunted-response-to-%C3%AE-blocker-therapy-using-carvedilol%C3%A3-insights-from-japanese-chronic-heart-failure-j-chf-study
#5
Yuji Nagatomo, Tsutomu Yoshikawa, Hiroshi Okamoto, Akira Kitabatake, Masatsugu Hori
BACKGROUND: Anemia portends a poor clinical outcome in patients with chronic heart failure (CHF). However, its mechanism remains unknown. We sought to elucidate the effect of anemia on patients with HF with reduced ejection fraction (HFrEF) who receive carvedilol therapy.Methods and Results:J-CHF study was a prospective, randomized, multicenter trial that assigned 360 HFrEF patients to 2.5 mg/5 mg/20 mg carvedilol groups according to the target dose. At baseline 70 patients (19%) had anemia ([A]) defined as hemoglobin level (Hb) <13 g/dL (male) or <12 g/dL (female) and the remaining 290 did not ([N])...
September 7, 2017: Circulation Journal: Official Journal of the Japanese Circulation Society
https://www.readbyqxmd.com/read/28882337/meta-analysis-comparing-metoprolol-and-carvedilol-on-mortality-benefits-in-patients-with-acute-myocardial-infarction
#6
Jingen Li, Zhuo Chen, Xiang Gao, He Zhang, Wenjing Xiong, Jianqing Ju, Hao Xu
Although carvedilol, a nonselective beta-blocker with alpha-adrenergic blocking and multiple ancillary activities, has been demonstrated to be superior to metoprolol in chronic heart failure, it remains unclear whether the superiority of carvedilol still exists in myocardial infarction (MI). Therefore, we performed a network meta-analysis of randomized controlled trials (RCTs) to compare the 2 drugs in patients with MI. All RCTs that compared either 2 of the following interventions, carvedilol, metoprolol, and placebo, for the treatment of MI were included...
July 29, 2017: American Journal of Cardiology
https://www.readbyqxmd.com/read/28877982/non-canonical-regulation-of-insulin-mediated-erk-activation-by-phosphoinositide-3-kinase-%C3%AE
#7
Maradumane L Mohan, Arunachal Chatterjee, Swetha Ganapathy, Sromona Mukherjee, Sowmya Srikanthan, George P Jolly, Rohit S Anand, Sathyamangla V Naga Prasad
Classically Class IB Phosphoinositide 3-kinase (PI3Kγ) plays a role in ERK activation following G-protein coupled receptor (GPCR) activation. Knock-down of PI3Kγ unsuspectingly resulted in loss of ERK activation to receptor tyrosine kinase-agonists like epidermal growth factor or insulin. Mouse embryonic fibroblasts (MEFs) or primary adult cardiac fibroblasts isolated from PI3Kγ knock-out mice (PI3KγKO) showed loss in insulin-stimulated ERK activation. However, expression of kinase-dead PI3Kγ resulted in rescue of insulin-stimulated ERK activation...
September 6, 2017: Molecular Biology of the Cell
https://www.readbyqxmd.com/read/28868298/case-report-of-spontaneous-remission-of-biopsy-proven-idiopathic-immune-complex-mediated-membranoproliferative-glomerulonephritis
#8
Rehan Shah, Mark S Segal, Michael J Wilkowski
Membranoproliferative glomerulonephritis (MPGN) is a histopathologic diagnosis causing microscopic hematuria, nephrotic range proteinuria, and chronic renal failure. Current understanding divides pathogenesis into two broad categories: immune complex mediated and complement mediated (now termed C3 glomerulopathy). The term idiopathic immune complex-mediated MPGN would apply to a patient without an identifiable source of immune complex production and no evidence of C3 glomerulopathy. Presented is a patient with idiopathic immune complex mediated MPGN and her clinical course...
May 2017: Case Reports in Nephrology and Dialysis
https://www.readbyqxmd.com/read/28862932/atrial-fibrillation-in-heart-failure-us-ambulatory-cardiology-practices-and-the-potential-for-uptake-of-catheter-ablation-an-national-cardiovascular-data-registry-ncdr-%C3%A2-research-to-practice-r2p-project
#9
Jehu S Mathew, Lucas N Marzec, Kevin F Kennedy, Philip G Jones, Paul D Varosy, Frederick A Masoudi, Thomas M Maddox, Larry A Allen
BACKGROUND: Atrial fibrillation (AF) and heart failure with reduced ejection fraction frequently coexist. The AATAC (Ablation versus Amiodarone for Treatment of persistent Atrial fibrillation in patients with Congestive heart failure and an implantable device) trial suggests that catheter ablation may benefit these patients. However, applicability to contemporary ambulatory cardiology practice is unknown. METHODS AND RESULTS: Using the outpatient National Cardiovascular Data Registry(®) Practice Innovation and Clinical Excellence Registry, we identified participants meeting AATAC enrollment criteria between 2013 and 2014...
August 11, 2017: Journal of the American Heart Association
https://www.readbyqxmd.com/read/28854816/carvedilol-inhibits-matrix-metalloproteinase-2-activation-in-experimental-autoimmune-myocarditis-possibilities-of-cardioprotective-application
#10
Monika Skrzypiec-Spring, Katarzyna Haczkiewicz, Agnieszka Sapa, Tomasz Piasecki, Joanna Kwiatkowska, Ireneusz Ceremuga, Mieczyslaw Wozniak, Wieslawa Biczysko, Christopher Kobierzycki, Piotr Dziegiel, Marzenna Podhorska-Okolow, Adam Szelag
AIMS: Acute myocarditis is a potentially lethal inflammatory heart disease that frequently precedes the development of dilated cardiomyopathy and subsequent heart failure. At present, there is no effective standardized therapy for acute myocarditis, besides the optimal care of heart failure and arrhythmias in accordance with evidence-based guidelines and specific etiology-driven therapy for infectious myocarditis. Carvedilol has been shown to be cardioprotective by reducing cardiac pro-inflammatory cytokines present in oxidative stress in certain heart diseases...
January 1, 2017: Journal of Cardiovascular Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/28821450/carvedilol-abrogates-hypoxia-induced-oxidative-stress-and-neuroinflammation-in-microglial-bv2-cells
#11
Xiujuan Gao, Bin Wu, Zhijian Fu, Zongwang Zhang, Guangjun Xu
Microglia initially undergo rapid activation in response to injury and stressful stimuli, such as hypoxia. Oxidative stress and the inflammatory response play critical roles in hypoxic-ischemic brain injury. Carvedilol is a β-blocker used to treat high blood pressure and heart failure. In this study, we investigated whether carvedilol had a protective effect against hypoxia-induced oxidative stress and inflammation in microglial BV2 cells. Our results indicate that hypoxic exposure significantly reduced mean cell viability of BV2 microglia, which was significantly restored by carvedilol (10 and 50μM)...
August 15, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28814664/pulmonary-arterial-hypertension-treatment-with-carvedilol-for-heart-failure-a-randomized-controlled-trial
#12
Samar Farha, Didem Saygin, Margaret M Park, Hoi I Cheong, Kewal Asosingh, Suzy Aa Comhair, Olivia R Stephens, Emir C Roach, Jacqueline Sharp, Kristin B Highland, Frank P DiFilippo, Donald R Neumann, W H Wilson Tang, Serpil C Erzurum
BACKGROUND: Right-sided heart failure is the leading cause of death in pulmonary arterial hypertension (PAH). Similar to left heart failure, sympathetic overactivation and β-adrenoreceptor (βAR) abnormalities are found in PAH. Based on successful therapy of left heart failure with β-blockade, the safety and benefits of the nonselective β-blocker/vasodilator carvedilol were evaluated in PAH. METHODS: PAH Treatment with Carvedilol for Heart Failure (PAHTCH) is a single-center, double-blind, randomized, controlled trial...
August 17, 2017: JCI Insight
https://www.readbyqxmd.com/read/28811301/topically-applied-carvedilol-attenuates-solar-ultraviolet-radiation-induced-skin-carcinogenesis
#13
Kevin M Huang, Sherry Liang, Steven Yeung, Etuajie Oiyemhonlan, Kristan H Cleveland, Cyrus Parsa, Robert Orlando, Frank L Meyskens, Bradley 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/28811130/comparative-study-on-stabilizing-ability-of-food-protein-non-ionic-surfactant-and-anionic-surfactant-on-bcs-type-ii-drug-carvedilol-loaded-nanosuspension-physicochemical-and-pharmacokinetic-investigation
#14
Tianjiao Geng, Parikshit Banerjee, Zhangdi Lu, Abdelmoumin Zoghbi, Tiantian Li, Bo Wang
Carvedilol (CAR) in its pure state has low aqueous solubility and extremely poor bioavailability which largely limit its clinical application. The aim of the study is to improve the dissolution rate and the bioavailability of CAR via preparing nanosuspensions with different stabilizers. Antisolvent precipitation-ultrasonication technique was used here. Attempts have been made to use food protein- Whey protein isolate (WPI) as a stabilizer in CAR loaded nanosuspension and also to compare its stabilizing potential with conventional nanosuspension stabilizers such as non-ionic linear copolymer-poloxamer 188 (PLX188) and anionic surfactant-sodium dodecyl sulfate (SDS)...
August 12, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28803116/efficient-molecularly-imprinted-polymer-as-a-pipette-tip-solid-phase-sorbent-for-determination-of-carvedilol-enantiomers-in-human-urine
#15
Anny Talita Maria da Silva, Hanna Leijoto de Oliveira, Camilla Fonseca Silva, Matheus Cecílio Fonseca, Thales Fernando Dias Pereira, Clebio Soares Nascimento, Eduardo Costa de Figueiredo, Keyller Bastos Borges
In this work, an efficient pipette tip based on molecularly imprinted polymers solid-phase extraction (PT-MIP-SPE) method was developed for carvedilol (CAR) analysis. This compound is available in clinical practice as a racemic mixture, in which (-)-(S)-CAR is a β- and α1-adrenergic antagonist, while (+)-(R)-CAR only acts as an α1-adrenergic antagonist. Enantioseparation of CAR presented satisfactory retention times (5.85 and 14.84min), acceptable theoretical plates (N=2048 and 2018) and good resolution (Rs=9...
September 1, 2017: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/28760606/synthesis-analytical-characterization-and-capillary-electrophoretic-use-of-the-single-isomer-heptakis-6-o-sulfobutyl-beta-cyclodextrin
#16
Milo Malanga, Ida Fejős, Erzsébet Varga, Gábor Benkovics, András Darcsi, Julianna Szemán, Szabolcs Béni
This contribution reports the synthesis, characterization and capillary electrophoretic application of heptakis-(6-O-sulfobutyl-ether)-β-cyclodextrin sodium salt, (6-(SB)7-β-CD). The compound was obtained through a five-steps synthesis and it represents the first example of single-isomer sulfobutylated cyclodextrin that carries the negatively charged functions exclusively on its primary side and it is unmodified on the lower rim. The purity of each intermediate was determined by appropriate liquid chromatographic methods, while the isomeric purity of the final product was established by an ad-hoc developed HPLC method based on a CD-Screen-IEC column...
July 21, 2017: Journal of Chromatography. A
https://www.readbyqxmd.com/read/28749696/influence-of-physiological-gastrointestinal-surfactant-ratio-on-the-equilibrium-solubility-of-bcs-class-ii-drugs-investigated-using-a-four-component-mixture-design
#17
Zhou Zhou, Claire Dunn, Ibrahim Khadra, Clive G Wilson, Gavin W Halbert
The absorption of poorly water-soluble drugs is influenced by the luminal gastrointestinal fluid content and composition, which control solubility. Simulated intestinal fluids have been introduced into dissolution testing including endogenous amphiphiles and digested lipids at physiological levels; however, in vivo individual variation exists in the concentrations of these components, which will alter drug absorption through an effect on solubility. The use of a factorial design of experiment and varying media by introducing different levels of bile, lecithin, and digested lipids has been previously reported, but here we investigate the solubility variation of poorly soluble drugs through more complex biorelevant amphiphile interactions...
August 22, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28748731/long-term-management-of-distinct-facial-flushing-and-persistent-erythema-of-rosacea-by-treatment-with-carvedilol
#18
Katharina Pietschke, Martin Schaller
BACKGROUND: The treatment of persistent erythema and flushing episodes in patients with rosacea remains a clinical challenge. A possible therapeutic option could be the use of antihypertensive drugs. OBJECTIVES: We therefore evaluated the effect of the non-selective β-blocker carvedilol in five Caucasian patients. METHODS: In a monocentric retrospective case study, the patients were treated with carvedilol titrated up to 12.5 mg twice a day over at least six months...
August 11, 2017: Journal of Dermatological Treatment
https://www.readbyqxmd.com/read/28733066/effective-use-of-levosimendan-in-anthracycline-induced-cardiomyopathy-a-case-report
#19
Nikolaos Miaris, Stefanos Zezas, Joseph Sgouros, Dimitra-Christina Zirou, Stefania Gkoura, George Stamoulis, Helen Angelopoulou, George Avgeropoulos, Epaminondas Samantas
BACKGROUND: Anthracycline-induced cardiomyopathy is a serious side effect that ranges from mild left ventricular systolic impairment to congestive heart failure and cardiogenic shock. Currently, there is no evidence indicating the effective use of levosimendan in these cases. OBJECTIVE: We aim to present a case of life-threatening doxorubicin-induced cardiomyopathy that was successfully managed with levosimendan. CASE: A 48-year-old female with formerly normal heart function, who had been treated with doxorubicin-based regimens for dedifferentiated chondrosarcoma, presented with cardiomyopathy with low left ventricular ejection fraction eight months after the last infusion...
July 18, 2017: Heart & Lung: the Journal of Critical Care
https://www.readbyqxmd.com/read/28732927/ultrasound-promoted-dispersive-micro-solid-phase-extraction-of-trace-anti-hypertensive-drugs-from-biological-matrices-using-a-sonochemically-synthesized-conductive-polymer-nanocomposite
#20
Maryam Hemmati, Maryam Rajabi, Alireza Asghari
In this work, a rapid and efficient procedure named ultrasound meliorated dispersive micro solid-phase extraction followed by high performance liquid chromatography-ultra violet detection (US-D-μSPE-HPLC-UV) was developed for the pre-concentration of the main trace anti-hypertensive drugs in complex matrices. The basis of this procedure was a polypyrrole-sodium dodecylbenzenesulfonate/zinc oxide (PPy-DBSNa/ZnO) nanocomposite. It was readily synthesized by the impressive way of in situ sonochemical oxidative polymerization in the presence of some additives such as FeCl3 and DBSNa, ultimately leading to the effective coating of PPy on the ZnO nanoparticle cores...
November 2017: Ultrasonics Sonochemistry
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