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https://www.readbyqxmd.com/read/28512729/protective-effects-of-nebivolol-against-interleukin-1%C3%AE-il-1%C3%AE-induced-type-ii-collagen-destruction-mediated-by-matrix-metalloproteinase-13-mmp-13
#1
Zhigang Li, Baoyi Liu, Dewei Zhao, BenJie Wang, Yupeng Liu, Yao Zhang, Fengde Tian, Borui Li
The pathological progression of osteoarthritis (OA) involves degradation of articular cartilage matrix. Type II collagen is the main component of cartilage matrix, which is degraded by pro-inflammatory cytokines such as IL-1β mediated by MMP-13. Nebivolol, a licensed drug used for the treatment of hypertension in clinics, displays its anti-inflammatory capacity in various conditions. However, whether Nebivolol has a protective effect on cartilage matrix degradation has not been reported before. In this study, we investigated the effects of Nebivolol on regulating the expression of MMP-13 and degradation of type II collagen...
May 17, 2017: Cell Stress & Chaperones
https://www.readbyqxmd.com/read/28509722/rationale-for-nebivolol-valsartan-combination-for-hypertension-review-of-preclinical-and-clinical-data
#2
Thomas D Giles, John R Cockcroft, Bertram Pitt, Abhijeet Jakate, Harold M Wright
: To treat hypertension, combining two or more antihypertensive drugs from different classes is often necessary. β-Blockers and renin-angiotensin-aldosterone system inhibitors, when combined, have been deemed 'less effective' based on partially overlapping mechanisms of action and limited evidence. Recently, the single-pill combination (SPC) of nebivolol (Neb) 5 mg - a vasodilatory β1-selective antagonist/β3 agonist - and valsartan 80 mg, an angiotensin II receptor blocker, was US Food and Drug Administration-approved for hypertension...
May 15, 2017: Journal of Hypertension
https://www.readbyqxmd.com/read/28498232/antihypertensive-drugs-aliskiren-nebivolol-and-olmesartan-reduce-hypertension-by-reducing-endothelial-microparticle-and-regulating-angiogenesis
#3
Moon Jain, Vivek Bhosale, Dipti Tripathi, Himalaya Singh, Niharika Pal, Kashif Hanif, Kumaravelu Jagavelu
The accelerated generation of endothelial microparticles (EMP) and impaired angiogenesis are the markers of vascular pathology during various cardiovascular and inflammatory conditions including hypertension. Since, studies comparing the effects of antihypertensive agents on these two parameters are limited; the present study was designed to compare the effects of three antihypertensive agents: aliskiren, nebivolol, and olmesartan, on the EMP generation and angiogenesis. Changes in the hemodynamic parameters and serum EMP count were determined post 3 weeks of the drug treatments [aliskiren (30 mg/kg), nebivolol (10 mg/kg), or olmesartan (5 mg/kg) per orally] in L-NAME induced rat model of hypertension...
May 9, 2017: Journal of Cardiovascular Pharmacology
https://www.readbyqxmd.com/read/28459657/investigation-of-a-potential-pharmacokinetic-interaction-between-nebivolol-and-fluvoxamine-in-healthy-volunteers
#4
Ana-Maria Gheldiu, Laurian Vlase, Adina Popa, Corina Briciu, Dana Muntean, Corina Bocsan, Anca Buzoianu, Marcela Achim, Ioan Tomuta, Ioana Todor, Maria Neag
PURPOSE: To investigate whether fluvoxamine coadministration can influence the pharmacokinetic properties of nebivolol and its active hydroxylated metabolite (4-OH-nebivolol) and to assess the consequences of this potential pharmacokinetic interaction upon nebivolol pharmacodynamics. METHODS: This open-label, non-randomized, sequential clinical trial consisted of two periods: Period 1 (Reference), during which each volunteer received a single dose of 5 mg nebivolol and Period 2 (Test), when a combination of 5 mg nebivolol and 100 mg fluvoxamine was given to all subjects, after a 6-days pretreatment regimen with fluvoxamine (50-100 mg/day)...
2017: Journal of Pharmacy & Pharmaceutical Sciences: a Publication of the Canadian Society for Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28456609/computational-modeling-for-cardiac-safety-pharmacology-analysis-contribution-of-fibroblasts
#5
Xin Gao, Tylor Engel, Brian E Carlson, Tetsuro Wakatsuki
INTRODUCTION: Drug-induced proarrhythmic potential is an important regulatory criterion in safety pharmacology. The application of in silico approaches to predict proarrhythmic potential of new compounds is under consideration as part of future guidelines. Current approaches simulate electrophysiology of a single human adult ventricular cardiomyocyte. However, drug-induced proarrhythmic potential can be different when cardiomyocytes are surrounded by non-muscle cells. Incorporating fibroblasts in models of myocardium is important particularly for predicting a drugs cardiac liability in the aging population - a growing population who take more medications and exhibit increased cardiac fibrosis...
April 26, 2017: Journal of Pharmacological and Toxicological Methods
https://www.readbyqxmd.com/read/28429695/lichenoid-type-cutaneous-hyperpigmentation-induced-by-nebivolol
#6
Abdullah Nabi Aslan, Murat Can Güney, Murat Akçay, Telat Keleş, Engin Bozkurt
Cutaneous hyperpigmentation is a common and well-defined side effect of many drugs, such as non-steroidal anti-inflammatory drugs, beta-blockers, and tetracyclines, but to the best of our knowledge there is no case of skin discoloration related to nebivolol in the literature. Presently described is lichenoid type cutaneous hyperpigmentation in a 46-year-old female patient. Hyperpigmentation emerged 3 months after initiating use of nebivolol and resolved after cessation of drug use. It was concluded that effect emerged as result of therapeutic doses of nebivolol...
April 2017: Türk Kardiyoloji Derneği Arşivi: Türk Kardiyoloji Derneğinin Yayın Organıdır
https://www.readbyqxmd.com/read/28423612/correction-nebivolol-a-%C3%AE-1-adrenergic-blocker-protects-from-peritoneal-membrane-damage-induced-during-peritoneal-dialysis
#7
Georgios Liappas, Guadalupe González-Mateo, Anna Rita Aguirre, Hugo Abensur, Patricia Albar-Vizcaino, Emilio González Parra, Pilar Sandoval, Laura García Ramírez, Gloria Del Peso, Juan Manuel Acedo, María A Bajo, Rafael Selgas, José A Sánchez Tomero, Manuel López-Cabrera, Abelardo Aguilera
No abstract text is available yet for this article.
April 4, 2017: Oncotarget
https://www.readbyqxmd.com/read/28405237/studies-directed-toward-the-exploitation-of-vicinal-diols-in-the-synthesis-of-nebivolol-intermediates
#8
Runjun Devi, Sajal Kumar Das
While the exploitation of the Sharpless asymmetric dihydroxylation as the source of chirality in the synthesis of acyclic molecules and saturated heterocycles has been tremendous, its synthetic utility toward chiral benzo-annulated heterocycles is relatively limited. Thus, in the search for wider applications of Sharpless asymmetric dihydroxylation-derived diols for the synthesis of benzo-annulated heterocycles, we report herein our studies in the asymmetric synthesis of (R)-1-((R)-6-fluorochroman-2-yl)ethane-1,2-diol, (R)-1-((S)-6-fluorochroman-2-yl)ethane-1,2-diol and (S)-6-fluoro-2-((R)-oxiran-2-yl)chroman, which have been used as late-stage intermediates for the asymmetric synthesis of the antihypertensive drug (S,R,R,R)-nebivolol...
2017: Beilstein Journal of Organic Chemistry
https://www.readbyqxmd.com/read/28387384/nebivolol-valsartan-fixed-dose-combination-for-treatment-of-hypertension
#9
D M Paton
Clinical trials demonstrated that a fixed-dose combination (FDC) of the beta-blocker nebivolol (5 mg) and the angiotensin II antagonist valsartan (80 mg) produced a significant reduction of both diastolic and systolic blood pressure in patients with hypertension. Both nebivolol and valsartan contributed to this effect, partial additivity of 86.6% and 82.2% being observed for diastolic and systolic blood pressure, respectively. These values are very similar to the additivity ratios of other recently approved FDCs for hypertension...
January 2017: Drugs of Today
https://www.readbyqxmd.com/read/28382958/role-of-nebivolol-in-the-control-and-management-of-central-aortic-blood-pressure-in-hypertensive-patients
#10
REVIEW
C Borghi, M C Acelajado, Y Gupta, S Jain
Measurement of blood pressure (BP) using a brachial cuff sphygmomanometer is universally accepted for the diagnosis of hypertension and prediction of cardiovascular diseases. However, brachial systolic BP does not represent actual systolic BP in the central arteries which encounter cardiac load directly. Due to wave amplification from central to peripheral arteries, a significant difference exists between the two. Central BP measurements also account for arterial stiffness, vessel branching and vascular mechanics, unlike brachial BP...
April 6, 2017: Journal of Human Hypertension
https://www.readbyqxmd.com/read/28375655/cardiopulmonary-exercise-test-as-a-tool-to-choose-therapy-in-heart-failure
#11
Mauro Contini
Heart failure treatment can count on several drugs, all providing an improvement in outcome, but that cannot be realistically used all together in the same patient. It would be useful to have a tool that allows arranging the most appropriate therapy cocktail in each patient. The aim of this review is to show the main differences in the effects of several drugs on cardiopulmonary function in heart failure patients, both in resting condition and during exercise, and to discuss how these differences can be taken into account when choosing the most appropriate therapeutic protocol...
April 4, 2017: Annals of the American Thoracic Society
https://www.readbyqxmd.com/read/28340419/photolytic-degradation-of-the-%C3%AE-blocker-nebivolol-in-aqueous-solution
#12
Alaa Salma, Holger V Lutze, Torsten C Schmidt, Jochen Tuerk
Nebivolol (NEB) is one of the top-sold prescription drugs belonging to the third generation of beta-blockers. However, so far, occurrence data in the environment are lacking. Within this study NEB has been found for the first time in effluent samples of wastewater treatment plants in Germany with an average concentration of 13 ng L(-1). Its photodegradation behavior in the environment and in technical processes is largely unknown. To fill this gap, three different UV treatment procedures (UV-C at 254 nm, UV-B at 312 nm and UV-A at 365 nm) were investigated in three different matrices: pure water, pure water in presence of the hydroxyl radical (OH) scavenger tert...
June 1, 2017: Water Research
https://www.readbyqxmd.com/read/28335640/nebivolol-attenuates-cerebral-vasospasm-both-by-increasing-endothelial-nitric-oxide-and-by-decreasing-oxidative-stress-in-an-experimental-subarachnoid-haemorrhage
#13
Mehmet Arif Aladag, Yusuf Turkoz, Hakan Parlakpinar, Mehmet Gul
OBJECTIVE: Evidence suggests that reduction of nitric oxide (NO) bioavailability due to oxidative stress plays a central role in the pathophysiology of cerebral vasospasm after subarachnoid haemorrhage (SAH). To prevent SAH-induced cerebral vasospasm, therefore we used nebivolol hydrochloride as a NO-mediated vasodilator and an antioxidant drug in an experimental rat model of SAH. MATERIALS AND METHODS: Forty female Wistar rats were divided into control, SAH, SAH plus placebo, and SAH plus nebivolol groups...
March 23, 2017: British Journal of Neurosurgery
https://www.readbyqxmd.com/read/28302931/the-comparison-of-the-effects-of-nebivolol-and-metoprolol-on-erectile-dysfunction-in-the-cases-with-coronary-artery-bypass-surgery
#14
Özcan Gür, Selami Gurkan, Gunduz Yumun, Polat Turker
PURPOSE: Beta-blocker use is common in the cases with coronary artery bypass surgery. According to the literature, beta-blockers have positive effects but may cause erectile dysfunction (ED). The most commonly used beta-blockers in ischemic cardiac disease are nebivolol and metoprolol. In our clinic, we aimed to compare the effects of nebivolol and metoprolol succinate on ED in the sexually active cases with coronary artery bypass surgery. METHODS: In our clinic, a total of 119 patients with coronary artery bypass surgery were included in the study...
April 20, 2017: Annals of Thoracic and Cardiovascular Surgery
https://www.readbyqxmd.com/read/28283926/differential-metabolic-effects-of-beta-blockers-an-updated-systematic-review-of-nebivolol
#15
REVIEW
Maria Marketou, Yashaswi Gupta, Shashank Jain, Panos Vardas
Blood pressure management in hypertensive patients with metabolic abnormalities is challenging, since many of the antihypertensive drugs adversely affect metabolism. Besides effective control of blood pressure in patients with hypertension, third-generation beta-blockers such as nebivolol offer additional benefits for central hemodynamics and neutral or beneficial effects on metabolism. Emerging clinical data suggest that nebivolol also has similar effects on metabolism in obese hypertensive and hypertensive diabetic patients...
March 2017: Current Hypertension Reports
https://www.readbyqxmd.com/read/28266722/development-and-validation-of-a-hplc-uv-method-for-the-simultaneous-determination-of-the-antipsychotics-clozapine-olanzapine-and-quetiapine-several-beta-blockers-and-their-metabolites
#16
Margarete Silva Gracia, Alexandra Köppl, Sandra Unholzer, Ekkehard Haen
A simple, accurate and selective column-switching high performance liquid chromatography (HPLC) method was developed and validated for simultaneous quantification of six beta-blockers (metoprolol MET, timolol TIM, bisoprolol BIS, propranolol PRO, carvedilol CAR and nebivolol NEB), three of their metabolites (α-hydroxy metoprolol α-HMET, N-desisopropyl propranolol DIPRO and 4'-hydroxy carvedilol 4-HCAR), three antipsychotics (olanzapine OLA, clozapine CLO and quetiapine QUE) and three of their metabolites (N-desmethyl olanzapine DMOLA, N-desmethyl clozapine DMCLO and N-desalkyl quetiapine DAQUE) in human serum...
March 7, 2017: Biomedical Chromatography: BMC
https://www.readbyqxmd.com/read/28252041/protective-effects-of-nebivolol-from-oxidative-stress-to-prevent-hypertension-related-target-organ-damage
#17
REVIEW
A Coats, S Jain
Hypertension is one of the leading risk factors for morbidity and mortality in patients with cardiovascular and cerebrovascular diseases and renal impairment. It also leads to target organ damage (TOD), which worsens organ function and the patient's clinical status. Reactive oxygen species (ROS)-mediated oxidative stress may contribute significantly to TOD in patients with hypertension. NO (nitric oxide) is a paracrine factor derived from endothelial cells that has been shown to alleviate ROS-mediated oxidative damage...
June 2017: Journal of Human Hypertension
https://www.readbyqxmd.com/read/28209351/an-indirect-stereoselective-analysis-of-nebivolol-glucuronides-in-plasma-by-lc-ms-ms-application-to-clinical-pharmacokinetics
#18
Carolina Pinto Vieira, Daniel Valente Neves, Evandro José Cesarino, Adriana Rocha, Séverine Poirier, Vera Lucia Lanchote
Nebivolol is a racemate of the d-isomer responsible for β1 adrenergic receptor antagonism and the l-isomer responsible for the release of nitric oxide from endothelial cells. Nebivolol is mainly metabolized to nebivolol glucuronide, which also contribute to the nebivolol β1 adrenoreceptor antagonism. This study reports the development and validation of an indirect stereoselective method of analysis of nebivolol glucuronides in plasma by LC-MS/MS. The method was applied to the investigation of stereoselectivity in the glucuronidation of nebivolol in elderly hypertensive patients (n=11) CYP2D6 phenotyped as EM and treated with a single oral dose of the racemate...
February 3, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28203288/nebivolol-versus-other-beta-blockers-in-patients-with-hypertension-and-erectile-dysfunction
#19
REVIEW
Randall P Sharp, Barry J Gales
Erectile dysfunction (ED) impacts over 100 million men worldwide and occurs at a higher incidence in men with hypertension. Beta blockers are one of several antihypertensive drug classes associated with ED. Nebivolol is a beta blocker with vasodilating properties mediated through endothelial release of nitric oxide which facilitates penile erection. Thus, nebivolol may offer an advantage over other beta blockers in the patient with hypertension and ED. A literature search comparing nebivolol with other beta blockers identified four European studies of limited duration, with the longest study being 28 weeks...
February 2017: Therapeutic Advances in Urology
https://www.readbyqxmd.com/read/28178754/neuroprotective-effect-of-nebivolol-against-cisplatin-associated-depressive-like-behavior-in-rats
#20
Noha F Abdelkader, Muhammed A Saad, Rania M Abdelsalam
One-third of cancer patients undergoing chemotherapy treatment often display symptoms of depression leading to poor adherence and decreased quality of life. Thus, this study aimed to investigate the possible protective effect of nebivolol against cisplatin-associated depressive symptoms in adult male rats. Nebivolol is a highly cardioselective β-adrenergic receptor blocker that possesses endothelium-dependent vasodilator properties and antioxidant capacities. Animals were allocated into four groups. Group one was given aqueous solution of carboxymethyl cellulose and served as control, group two was given nebivolol (10 mg/kg p...
May 2017: Journal of Neurochemistry
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