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https://www.readbyqxmd.com/read/29676238/effect-of-cyp2d6-poor-metabolizer-phenotype-on-stereoselective-nebivolol-pharmacokinetics
#1
Carolina P Vieira, Daniel V Neves, Eduardo B Coelho, Vera Lucia Lanchote
BACKGROUND: Nebivolol is a drug available as a racemate of d-nebivolol (SRRR) and l-nebivolol (RSSS). In human liver microsomes CYP2D6 mainly catalyses the metabolism of l-nebivolol, while CYP2C19 catalyses the metabolism of d-nebivolol. Nebivolol stereoselective pharmacokinetics has been described only for extensive metabolizers (EM). OBJECTIVE: To describe the stereoseletive nebivolol pharmacokinetics in CYP2D6 poor metabolizers (PM) and to assess whether the phenotype has an impact on nebivolol pharmacokinetics ...
April 19, 2018: Drug Metabolism Letters
https://www.readbyqxmd.com/read/29618986/the-antioxidant-therapy-new-insights-in-the-treatment-of-hypertension
#2
REVIEW
Daniela Sorriento, Nicola De Luca, Bruno Trimarco, Guido Iaccarino
Reactive oxygen species (ROS) and reactive nitrogen species (RNS) play a key role in the regulation of the physiological and pathological signaling within the vasculature. In physiological conditions, a delicate balance between oxidants and antioxidants protects cells from the detrimental effects of ROS/RNS. Indeed, the imbalance between ROS/RNS production and antioxidant defense mechanisms leads to oxidative and nitrosative stress within the cell. These processes promote the vascular damage observed in chronic conditions, such as hypertension...
2018: Frontiers in Physiology
https://www.readbyqxmd.com/read/29513811/investigation-of-the-antioxidant-effects-of-pheniramine-maleate-and-nebivolol-on-testicular-damage-in-rats-with-experimentally-induced-testis-torsion
#3
Ercan Yuvanc, Devrim Tuglu, Tunc Ozan, Ucler Kisa, Mahi Balci, Ertan Batislam, Erdal Yilmaz
PURPOSE: To investigate the biochemical, histopathologic, and spermatogenetic changes in the detorsionated testicle after experimental torsion and to study the antioxidant effects of pheniramine maleate and nebivolol. METHODS: Twenty-four Sprague-Dawley male rats were divided into 4 groups: Group 1: Sham; Group 2: Torsion/Detorsion (T/D); Group 3: T/D + Pheniramine maleate (PM); Group 4: T/D + Nebivolol (NB) group. Paroxanase (PON), total antioxidant status (TAS), total oxidant status (TOS), and oxidative stres index (OSI) were measured, and spermatogenetic and histopathologic evaluation was performed in tissue and blood samples...
February 2018: Acta Cirúrgica Brasileira
https://www.readbyqxmd.com/read/29413973/novel-bio-analytical-method-development-validation-and-application-for-simultaneous-determination-of-nebivolol-and-s-amlodipine-in-human-plasma-using-ultra-performance-liquid-chromatography-tandem-mass-spectrometry
#4
Bhargav M Patel, Arvind G Jangid, B N Suhagia, Nirmal Desai
A sensitive and specific ultra-performance liquid chromatography tandem mass spectrometric (UPLC-MS/MS) method has been developed, validated and applied for the assay of Nebivolol and S-amlodipine in human plasma. Sample extraction was carried out through hybrid extraction method from 250 μL of human plasma sample. Linearity of the method was (r ≥ 0.9996) was found to be dynamic for both the analytes over concentration range of 25.0-4000 pg/mL. Chromatographic separation was achieved on UPLC column {Waters Acquity UPLC BEH C18 (50 mm × 2...
January 6, 2018: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/29408764/protective-role-of-nebivolol-in-cadmium-induced-hepatotoxicity-via-downregulation-of-oxidative-stress-apoptosis-and-inflammatory-pathways
#5
Marwa M M Refaie, Maram El-Hussieny, Nagwa M Zenhom
Cadmium (Cd) intoxication in human occurs through inhalation of cigarette smoke and ingestion of contaminated water and food. We investigated the role of nebivolol (NEB) in Cd induced hepatotoxicity. In our study; NEB was given as (10 mg/kg/d) orally to rats for 6 weeks, in the presence or absence of hepatotoxicity induced by oral administration of Cd (7 mg/kg/d) for 6 weeks. Levels of serum liver enzyme biomarkers; alanine transaminase (ALT), aspartate transaminase (AST) and serum total antioxidant capacity (TAC) were measured...
March 2018: Environmental Toxicology and Pharmacology
https://www.readbyqxmd.com/read/29389578/a-novel-uv-photolysis-approach-with-acetone-and-isopropyl-alcohol-for-the-rapid-determination-of-fluoride-in-organofluorine-containing-drugs-by-spectrophotometry
#6
Venkata Balarama Krishna Mullapudi, Karunasagar Dheram
A UV photolysis decomposition (UVPD) method for the determination of fluoride in fluorine containing pharmaceuticals by spectrophotometry is reported. It is based on the use of high intensity UV-irradiation in the presence of a digesting solution comprising a mixture of acetone and isopropanol. For the optimization of the UVPD procedure, three bulk drugs (levofloxacin, nebivolol and efavirenz) were chosen as representatives of three diverse compounds containing a single fluorine atom, two fluorine atoms, and trifluoromethyl groups respectively...
January 2018: Journal of Food and Drug Analysis
https://www.readbyqxmd.com/read/29365224/nebivolol-valsartan-byvalson-for-hypertension
#7
Nathan H Lamberton, Ardis M Copenhaver
No abstract text is available yet for this article.
January 15, 2018: American Family Physician
https://www.readbyqxmd.com/read/29362613/protective-effects-of-the-third-generation-vasodilatory-%C3%AE-eta-blocker-nebivolol-against-d-galactosamine-induced-hepatorenal-syndrome-in-rats
#8
Ahmed Atwa, Rehab Hegazy, Rania Mohsen, Neamat Yassin, Sanaa Kenawy
BACKGROUND: Renal dysfunction is very common in patients with advanced liver cirrhosis and portal hypertension. The development of renal failure in the absence of clinical, anatomical or pathological causes renal of failure is termed hepatorenal syndrome (HRS). AIM: The present study was constructed to investigate the possible protective effects of nebivolol (Nebi) against D-galactosamine (Gal)-induced HRS in rats. MATERIAL AND METHODS: Rats were treated with Nebi for ten successive days...
December 15, 2017: Open Access Macedonian Journal of Medical Sciences
https://www.readbyqxmd.com/read/29337670/sustained-release-biodegradable-solid-lipid-microparticles-formulation-evaluation-and-statistical-optimization-by-response-surface-methodology
#9
Muhammad Hanif, Hafeez Ullah Khan, Samina Afzal, Asif Mahmood, Safirah Maheen, Khurram Afzal, Nabila Iqbal, Mehwish Andleeb, Nazar Abbas
For preparing nebivolol loaded solid lipid microparticles (SLMs) by the solvent evaporation microencapsulation process from carnauba wax and glyceryl monostearate, central composite design was used to study the impact of independent variables on yield (Y1), entrapment efficiency (Y2) and drug release (Y3). SLMs having a 10-40 μm size range, with good rheological behavior and spherical smooth surfaces, were produced. Fourier transform infrared spectroscopy, differential scanning calorimetry and X-ray diffractometry pointed to compatibility between formulation components and the zeta-potential study confirmed better stability due to the presence of negative charge (-20 to -40 mV)...
December 20, 2017: Acta Pharmaceutica
https://www.readbyqxmd.com/read/29322226/nebivolol-a-%C3%AE-blocker-abrogates-streptozotocin-induced-behavioral-biochemical-and-neurophysiological-deficit-by-attenuating-oxidative-nitrosative-stress-a-possible-target-for-the-prevention-of-diabetic-neuropathy
#10
Naini Bhadri, Rema Razdan, Sumanta Kumar Goswami
Metabolic abnormalities including hyperglycemia, hyperlipidemia, and oxidative-nitrosative stress are involved in the progression of diabetic neuropathy. In the present study, we targeted oxidative-nitrosative stress using nebivolol, a β1 -receptor antagonist with vasodilator and antioxidant property, to evaluate its neuroprotective effect in streptozotocin-induced diabetic neuropathy in rats. Diabetic neuropathy develops within 4-6 weeks after administration of streptozotocin (55 mg/kg, i.p.). Therefore, after confirmation of diabetes, subtherapeutic doses of nebivolol (1 and 2 mg/kg, p...
February 2018: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/29319332/nebivolol-attenuates-oxidative-stress-and-inflammation-in-a-guinea-pig-model-of-ovalbumin-induced-asthma-a-possible-mechanism-for-its-favorable-respiratory-effects
#11
Sally A Abuelezz
An experimental model of ovalbumin (OVA) induced asthma was used to assess the effects of nebivolol, the third-generation selective β1 -adrenergic receptor blocker, on airway reactivity, lung inflammation, and oxidative stress markers. The asthma induction protocol was done by OVA sensitization and challenge. Guinea pigs were classified into control, asthmatic, or asthmatic receiving nebivolol either 7.5 or 15 mg·kg-1 ·day-1 orally. At the end of the study respiratory, the anti-inflammatory and antioxidative effects of nebivolol were assessed...
March 2018: Canadian Journal of Physiology and Pharmacology
https://www.readbyqxmd.com/read/29184167/effect-of-nebivolol-or-atenolol-vs-placebo-on-cardiovascular-health-in-subjects-with-borderline-blood-pressure-the-evidence-study
#12
Daniel A Duprez, Natalia Florea, Sue Duval, Catherine Koukol, Jay N Cohn
Pharmacotherapy to protect the arteries may be appropriate for individuals with high-normal blood pressure who are at risk for future cardiovascular disease (CVD). Nebivolol (NEB) in contrast to atenolol (ATE) may have a beneficial effect on endothelial function and may be more effective than ATE in preventing CVD. Sixty subjects with preHTN or borderline BP and abnormal small artery elasticity (SAE) underwent evaluation with 10 tests, including large and small artery elasticity, resting and treadmill exercise BP, carotid intimal-media thickness, retinal vascular photography, micro-albuminuria, electrocardiography, echocardiography, and plasma B-type natriuretic peptide level...
December 2017: Journal of Human Hypertension
https://www.readbyqxmd.com/read/29159953/relationship-between-heart-failure-concurrent-chronic-obstructive-pulmonary-disease-and-beta-blocker-use-a-danish-nationwide-cohort-study
#13
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...
March 2018: European Journal of Heart Failure
https://www.readbyqxmd.com/read/29122812/nebivolol-but-not-metoprolol-treatment-improves-endothelial-fibrinolytic-capacity-in-adults-with-elevated-blood-pressure
#14
Brian L Stauffer, Caitlin A Dow, Kyle J Diehl, Tyler D Bammert, Jared J Greiner, Christopher A DeSouza
BACKGROUND: Vascular endothelial fibrinolytic function is impaired in adults with prehypertension and hypertension and plays a mechanistic role in the development of atherothrombotic events. The influence of β-blockers on endothelial fibrinolysis is unknown. This study compared the effects of chronic nebivolol and metoprolol treatment on endothelial tissue-type plasminogen activator (t-PA) release in adults with elevated blood pressure (BP). METHODS AND RESULTS: Forty-four middle-aged adults (36% women) with elevated BP completed a 3-month, double-blind, randomized, placebo-controlled trial comparing nebivolol (5 mg/d), metoprolol succinate (100 mg/d), and placebo...
November 9, 2017: Journal of the American Heart Association
https://www.readbyqxmd.com/read/29117660/nebivolol-induced-hyperkalemia-case-report
#15
Karmela Altabas, Velimir Altabas, Tonko Gulin
In this article, we document a conclusive case of nebivolol-induced hyperkalemia for the first time in the known medical literature. Hyperkalemia is associated with serious conditions such as cardiac arrhythmias and sudden cardiac death. Nebivolol was not known to cause hyperkalemia, and this event is not listed in its summary of product characteristics (SmPC). For older beta blockers, hyperkalemia is recognized as a rare adverse event linked to cytochrome P450 2D6 (CYP2D6) polymorphism and poor drug degradation...
December 2016: Acta Clinica Croatica
https://www.readbyqxmd.com/read/29105958/additivity-of-nebivolol-valsartan-single-pill-combinations-versus-other-single-pill-combinations-for-hypertension
#16
Jack Ishak, Michael Rael, Henry Punzi, Alan Gradman, Lynn M Anderson, Mehul Patel, Sanjida Ali, William Ferguson, Joel Neutel
The single-pill combination (SPC) comprising nebivolol (5 mg), a vasodilatory β1 -selective antagonist/β3 -agonist, and valsartan (80 mg), a renin-angiotensin-aldosterone system inhibitor, is the only Food and Drug Administration-approved β-blocker/renin-angiotensin-aldosterone system inhibitor SPC for hypertension. Additive effects of four nebivolol/valsartan SPC doses (5 mg/80 mg, 5/160 mg, 10/160 mg, 10/320 mg nebivolol/valsartan) were compared with five Food and Drug Administration-approved non-β-blocker/renin-angiotensin-aldosterone system inhibitor SPCs (aliskiren/hydrochlorothiazide, aliskiren/amlodipine, valsartan/amlodipine, aliskiren/valsartan, and telmisartan/amlodipine)...
January 2018: Journal of Clinical Hypertension
https://www.readbyqxmd.com/read/29098786/functional-characterization-of-cyp2c19-variants-in-nebivolol-4-hydroxlation-in-vitro
#17
Xiao-Yang Zhou, Xiao-Xia Hu, Meng-Fang Li, Hao Wang, Li-Qun Zhang, Guo-Xin Hu, Jian-Ping Cai
Cytochrome P450 2C19 (CYP2C19) allelic variants are thought to play an important part in inter-individual variability in drug metabolism. We evaluated the in vitro hydroxylation of nebivolol by 31 CYP2C19 alleles identified in a Chinese Han population recently. Wild-type CYP2C19*1B and 30 isoforms were highly expressed in insect cells, and the enzymatic activities of CYP2C19 variants towards nebivolol hydroxylation were characterized. Among the 30 CYP2C19 alleles, most of the recombinant CYP2C19 variants exhibited no or significantly low activity compared with CYP2C19*1B...
November 3, 2017: Drug Testing and Analysis
https://www.readbyqxmd.com/read/29068591/effect-of-nebivolol-on-fracture-healing-an-experimental-rat-model
#18
Hasan Metineren, Turan Cihan Dülgeroğlu, Mehmet Hüseyin Metineren, Ekrem Aydın
BACKGROUND: Bone metabolism is a complex system, and fracture healing is one of its most important functions. Many circumstances can influence this process. Chronic drug use in elderly populations can affect bone healing, and inadequate tissue perfusion, increased free radicals and adverse drug effects can negatively influence fracture healing. Nebivolol, an anti-hypertensive drug that selectively blocks β1 receptors, effectively reduces blood pressure by inducing peripheral vasodilation...
September 2017: Advances in Clinical and Experimental Medicine: Official Organ Wroclaw Medical University
https://www.readbyqxmd.com/read/28911302/what-is-the-real-efficacy-of-beta-blockers-for-the-treatment-of-essential-hypertension
#19
Christian Hocht, 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 β-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 β-blockers for the treatment of uncomplicated hypertension to second and third line therapy...
2017: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/28819568/nebivolol-attenuates-neutrophil-lymphocyte-ratio-a-marker-of-subclinical-inflammation-in-hypertensive-patients
#20
Mazhar Hussain, Muhammad Saeed, Muhammad Zafar Majeed Babar, Moazzam Ali Atif, Lubna Akhtar
BACKGROUND: High value of neutrophil lymphocyte ratio (NLR) is a strong independent predictor and biomarker of ongoing vascular inflammation in various cardiovascular disorders. OBJECTIVE: The main focus of the study is to investigate the effect of nebivolol on NLR in mild to moderate hypertensive patients in comparison with metoprolol. In addition, BMI, blood pressure, TLC count, blood sugar, and lipid profile were also assayed before and after treatment. MATERIALS AND METHODS: In this 12-week prospective double-blinded randomized study, 120 patients with mild to moderate hypertension were randomly divided into two groups to prescribed daily dose of tab nebivolol 5-10 mg and metoprolol 50-100 mg, respectively, for 12 weeks...
2017: International Journal of Hypertension
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