N-aryl amides as chemical exchange saturation transfer magnetic resonance imaging contrast agents.
Abstract Chemical exchange saturation transfer (CEST) MRI has recently emerged as a versatile molecular imaging approach in which diamagnetic compounds can be utilized to generate MRI signal. To expand the scope of CEST MRI applications, herein, we systematically investigated the CEST properties of N-aryl amides with different N-aromatic substitution, revealing their chemical shifts (4.6-5.8 ppm) and exchange rates (up to thousands s -1 ) are favorable to be used as CEST agents as compared to alkyl amide. As the first proof-of-concept study, we used CEST MRI to detect the enzymatic metabolism of the drug acebutolo...
Source: Chemistry - July 8, 2020 Category: Chemistry Authors: Cai X, Zhang J, Lu J, Yi L, Han Z, Zhang S, Yang X, Liu G Tags: Chemistry Source Type: research

Enantiospecific behaviour of chiral drugs in soil.
Abstract The importance of stereochemistry on the behaviour and effects of chiral pharmaceutical and illicit drugs in amended agricultural soils has been over looked to date. Therefore, this study was aimed at investigating the enantiospecific behaviour of a chemically diverse range of chiral drugs including naproxen, ibuprofen, salbutamol, bisoprolol, metoprolol, propranolol, acebutolol, atenolol, chlorpheniramine, amphetamine, fluoxetine and citalopram in soil microcosms. Considerable changes of the enantiomeric composition of ibuprofen, naproxen, atenolol, acebutolol and amphetamine were observed within 56 ...
Source: Environmental Pollution - May 25, 2020 Category: Environmental Health Authors: Bertin S, Yates K, Petrie B Tags: Environ Pollut Source Type: research

Drugs for Hypertension
Date: May 18, 2020 Issue #:  1598Summary:  Drugs available for treatment of chronic hypertension and their dosages, adverse effects, and costs are listed in the tables. Treatment of hypertensive urgencies and emergencies is not discussed here. (Source: The Medical Letter)
Source: The Medical Letter - April 29, 2020 Category: Drugs & Pharmacology Authors: admin Tags: Accupril Accuretic ACE inhibitors Acebutolol Adalat Aldactone aliskiren Altace Amiloride Amlodipine ARBs Atacand Atenolol Avalide Avapro azilsartan benazapril Benicar Beta blockers Betaxolol Bisoprolol Bumetanide Source Type: research

Chiral separation of beta-blockers by high-performance liquid chromatography and determination of bisoprolol enantiomers in surface waters.
E, Galić N Abstract Beta-blockers are chiral compounds with enantiomers that have different bioactivity, which means that while one is active, the other can be inactive or even harmful. Due to their high consumption and incomplete degradation in waste water, they may reach surface waters and affect aquatic organisms. To address this issue we developed a chromatographic method suitable for determining beta-blocker enantiomers in surface waters. It was tested on five beta-blockers (acebutolol, atenolol, bisoprolol, labetalol and metoprolol) and validated on bisoprolol enantiomers. Good enantioseparation of all anal...
Source: Arhiv za Higijenu Rada i Toksikologiju - March 1, 2020 Category: Occupational Health Authors: Pocrnić M, Ansorge M, Dovhunová M, Habinovec I, Tesařová E, Galić N Tags: Arh Hig Rada Toksikol Source Type: research

Stereoselective cell uptake of adrenergic agonists and antagonists by organic cation transporters.
r J Abstract Stereoselectivity is well described for receptor binding and enzyme catalysis, but so far has only been scarcely investigated in carrier-mediated membrane transport. We thus studied transport kinetics of racemic (anti)adrenergic drugs by the organic cation transporters OCT1 (wild-type and allelic variants), OCT2, OCT3, MATE1, and MATE2-K with a focus on stereospecificity. OCT1 showed stereoselective uptake with up to 2-fold higher vmax over their corresponding counterpart enantiomers for (R,R)-fenoterol, (R,R)-formoterol, (S)-salbutamol, (S)-acebutolol, and (S)-atenolol. Orciprenaline and etilefrine w...
Source: Biochemical Pharmacology - November 26, 2019 Category: Drugs & Pharmacology Authors: Jensen O, Rafehi M, Tzvetkov MV, Brockmöller J Tags: Biochem Pharmacol Source Type: research

Molecules, Vol. 24, Pages 3664: Graphene Oxide/Polyethylene Glycol-Stick for Thin Film Microextraction of β-Blockers from Human Oral Fluid by Liquid Chromatography-Tandem Mass Spectrometry
Molecules, Vol. 24, Pages 3664: Graphene Oxide/Polyethylene Glycol-Stick for Thin Film Microextraction of β-Blockers from Human Oral Fluid by Liquid Chromatography-Tandem Mass Spectrometry Molecules doi: 10.3390/molecules24203664 Authors: Hanieh Karimiyan Mohammad Reza Hadjmohammadi Karthik Laxman Kunjali Mohammad Mahdi Moein Joydeep Dutta Mohamed Abdel-Rehim A wooden stick coated with a novel graphene-based nanocomposite (Graphene oxide/polyethylene glycol (GO/PEG)) is introduced and investigated for its efficacy in solid phase microextraction techniques. The GO/PEG-stick was prepared and subsequent...
Source: Molecules - October 11, 2019 Category: Chemistry Authors: Hanieh Karimiyan Mohammad Reza Hadjmohammadi Karthik Laxman Kunjali Mohammad Mahdi Moein Joydeep Dutta Mohamed Abdel-Rehim Tags: Article Source Type: research

Perioperative beta-blockers for preventing surgery-related mortality and morbidity in adults undergoing cardiac surgery.
CONCLUSIONS: We found no evidence of a difference in early all-cause mortality, myocardial infarction, cerebrovascular events, hypotension and bradycardia. However, there may be a reduction in atrial fibrillation and ventricular arrhythmias when beta-blockers are used. A larger sample size is likely to increase the certainty of this evidence. Four studies awaiting classification may alter the conclusions of this review. PMID: 31544227 [PubMed - as supplied by publisher] (Source: Cochrane Database of Systematic Reviews)
Source: Cochrane Database of Systematic Reviews - September 23, 2019 Category: General Medicine Authors: Blessberger H, Lewis SR, Pritchard MW, Fawcett LJ, Domanovits H, Schlager O, Wildner B, Kammler J, Steinwender C Tags: Cochrane Database Syst Rev Source Type: research

Choice of anti-hypertensive treatment in HELLP syndrome at ehu Oran
ConclusionThe management of hypertension was done according to a codified protocol with molecules available in each Maghreb establishment; it requires deep involvement of the paramedical staff. (Source: Archives of Cardiovascular Diseases Supplements)
Source: Archives of Cardiovascular Diseases Supplements - July 24, 2019 Category: Cardiology Source Type: research

Analysis of beta-blocker bioconcentration in brown planaria (Girardia dorotocephala) and its effects on regeneration.
Abstract Production, distribution, and disposal of pharmaceutical products, including beta-blockers, have become a global issue. Beta-blockers are known to persist in the environment months after their release and may result in the disruption of the homeostatic system in non-target organisms. Here, we study the bioconcentration of three of the most commonly used beta-blockers and their effect on the regeneration of Girardia dorotocephala, a freshwater brown planarian. Acute toxicity tests determined LC50s for acebutolol, metoprolol, and propranolol to be 778 mg/L, 711 mg/L, and 111 mg/L, respectively. The qua...
Source: Environmental Science and Pollution Research International - July 20, 2019 Category: Environmental Health Authors: AminiTabrizi R, Hassan D, Davis R, Tucker KR Tags: Environ Sci Pollut Res Int Source Type: research

Structural and energetic evolution of fibrinogen toward to the betablocker interactions.
We present a computational analysis coupled with experimental studies, focusing on the binding-interaction between beta-adrenoreceptor blocking agents (acebutolol and propranolol) with fibrinogen protein (E-region). Herein, computational modeling on structural validation and flexibility properties of fibrinogen E-region showed that the E-region interacting residues, which form the funnel-shaped hydrophobic cavity for ligand-binding, can be efficiently modeled. The obtained free energy of binding (FEB) values for the docking complexes, namely acebutolol/fibrinogen E-region and propranolol/fibrinogen E-region, were very clos...
Source: International Journal of Biological Macromolecules - June 29, 2019 Category: Biochemistry Authors: González-Durruthy M, Scanavachi G, Rial R, Liu Z, Cordeiro MNDS, Itri R, Ruso JM Tags: Int J Biol Macromol Source Type: research

Correction to: A case of fatal acebutolol poisoning: an illustration of the potential of molecular networking
The published version of this article unfortunately contained a mistake. In Figure 1 on the molecular network of acebutololol, two molecular structures are not displayed ( “acebutolol glucuronide “and “impurity J”). The Figure is corrected here. (Source: International Journal of Legal Medicine)
Source: International Journal of Legal Medicine - May 24, 2019 Category: Medical Law Source Type: research

Effect of cavitation erosion in the sonochemical exfoliation of activated graphite for electrocatalysis of acebutolol.
This study mainly covered the cavitation erosion in probe sonication and its electrochemical behavior. The activated graphite was exfoliated by the probe sonication wherein the titanium alloy (TA) is used as a probe (micro-tip). The sonication performed in the aqueous solution contains a mixture of sulfuric acid and nitric acid (1:1). The exfoliated graphite (EG) was examined by field emission scanning electron microscope, Raman and X-ray diffraction pattern analysis. The results showed that some TA particles dissolute from the TA micro-tip accompanied with graphite exfoliation. This dissolution experienced from the cavita...
Source: Ultrasonics Sonochemistry - May 20, 2019 Category: Chemistry Authors: Karikalan N, Elavarasan M, Yang TCK Tags: Ultrason Sonochem Source Type: research

Droplet flow-assisted heterogeneous electro-Fenton reactor for degradation of beta-blockers: response surface optimization, and mechanism elucidation.
In this study, we report an effective degradation method for trace level beta-blockers (propranolol and acebutolol) in hospital wastewater using a new droplet flow-assisted heterogeneous electro-Fenton reactor (DFEF) system. Biogenic iron-carbon nanocomposites (RHS/C-x% Fe) as eco-friendly and low-cost heterogeneous Fenton catalysts were synthesized from rice husk via hydrolytic sol-gel routes. Here, we demonstrate the use of natural air as a nebulizing agent for fast and continuous catholyte air saturation and Fenton catalyst transfer to the cathode electrode. The effects of key operational parameters were evaluated and o...
Source: Environmental Science and Pollution Research International - March 12, 2019 Category: Environmental Health Authors: Nsubuga H, Basheer C, Jalilov A, Haider MB, Al-Saadi AA Tags: Environ Sci Pollut Res Int Source Type: research

Nature of intramolecular dynamics in protic ionic glass-former: insight from ambient and high pressure Brillouin spectroscopy
Publication date: Available online 28 February 2019Source: Journal of Molecular LiquidsAuthor(s): M. Pochylski, J. Gapiński, Z. Wojnarowska, M. Paluch, A. PatkowskiAbstractProton conducting materials play an important role in a variety of electrochemical devices. Especially, the class of protic ionic glass-formers with fast water-independent proton transport within the Grotthuss mechanism has been envisioned as promising fuel cell electrolytes. Nevertheless, despite a number of reports on protic ionic glasses the description of proton transport phenomenon in these systems is still incomplete. Herein, we employed the Brill...
Source: Journal of Molecular Liquids - February 28, 2019 Category: Molecular Biology Source Type: research

Dispersive solid-phase extraction using multi-walled carbon nanotubes combined with liquid chromatography–mass spectrometry for the analysis of β-blockers: Experimental and theoretical studies
Publication date: May 2019Source: Microchemical Journal, Volume 146Author(s): Aleksandra Jakubus, Maciej Gromelski, Karolina Jagiello, Tomasz Puzyn, Piotr Stepnowski, Monika PaszkiewiczAbstractThis manuscript presents a dispersive solid phase extraction (dSPE) method combined with liquid chromatography mass spectrometry (LC-MS/MS) to simultaneous determination and quantification of six β-blockers in environmental water samples. The proposed method is based on a multi-walled carbon nanotubes (MWCNTs) as a sorbent, because of their remarkable sorption capacity. Crucial parameters which may affect extraction efficiency s...
Source: Microchemical Journal - January 15, 2019 Category: Chemistry Source Type: research

Migraine Headache Prophylaxis.
Abstract Migraines impose significant health and financial burdens. Approximately 38% of patients with episodic migraines would benefit from preventive therapy, but less than 13% take prophylactic medications. Preventive medication therapy reduces migraine frequency, severity, and headache-related distress. Preventive therapy may also improve quality of life and prevent the progression to chronic migraines. Some indications for preventive therapy include four or more headaches a month, eight or more headache days a month, debilitating headaches, and medication-overuse headaches. Identifying and managing environmen...
Source: American Family Physician - January 1, 2019 Category: Primary Care Authors: Ha H, Gonzalez A Tags: Am Fam Physician Source Type: research

Simultaneous determination of pindolol, acebutolol and metoprolol in waters by differential-pulse voltammetry using an efficient sensor based on carbon paste electrode modified with amino-functionalized mesostructured silica
Publication date: 15 March 2019Source: Sensors and Actuators B: Chemical, Volume 283Author(s): Mariana Silva, Sonia Morante-Zarcero, Damián Pérez-Quintanilla, Isabel SierraAbstractIn this work, hexagonal mesoporous silica (HMS) and amino-functionalized HMS (HMS-NH2) were prepared and incorporated into carbon paste electrodes (CPEs) to obtain electrochemical sensors for pindolol (Pin), acebutolol (Ace) and metoprolol (Met) determination in waters by voltammetric techniques. The materials were characterized and they showed high specific surface area, large pore volume and a quasi-spherical morphology. Firstly, ...
Source: Sensors and Actuators B: Chemical - December 18, 2018 Category: Chemistry Source Type: research

LC and LC–MS/MS studies for the identification and characterization of degradation products of acebutolol
Publication date: Available online 15 March 2018Source: Journal of Pharmaceutical AnalysisAuthor(s): Uday Rakibe, Ravi Tiwari, Anand Mahajan, Vipul Rane, Pravin WakteAbstractThe aim of the present investigation was to demonstrate an approach involving use of liquid chromatography (LC) and liquid chromatography-mass spectrometry (LC–MS) to separate, identify and characterize very small quantities of degradation products (DPs) of acebutolol without their isolation from the reaction mixtures. The drug was subjected to oxidative, hydrolytic, thermal and photolytic stress conditions as per International Conference on Harm...
Source: Journal of Pharmaceutical Analysis - July 10, 2018 Category: Drugs & Pharmacology Source Type: research

LC and LC–MS/MS studies for the identification and characterization of degradation products of acebutalol
Publication date: Available online 15 March 2018Source: Journal of Pharmaceutical AnalysisAuthor(s): Uday Rakibe, Ravi Tiwari, Anand Mahajan, Vipul Rane, Pravin WakteAbstractThe aim of the present investigation was to demonstrate an approach involving use of liquid chromatography (LC) and liquid chromatography-mass spectrometry (LC-MS) analytical techniques to separate, identify and characterize very small quantities of degradation products (DPs) of acebutolol without their isolation from the reaction mixtures. The drug was subjected to oxidative, hydrolytic, thermal and photolytic stress conditions as per International Co...
Source: Journal of Pharmaceutical Analysis - July 5, 2018 Category: Drugs & Pharmacology Source Type: research

LC and LC –MS/MS studies for the identification and characterization of degradation products of acebutalol
Publication date: Available online 15 March 2018 Source:Journal of Pharmaceutical Analysis Author(s): Uday Rakibe, Ravi Tiwari, Anand Mahajan, Vipul Rane, Pravin Wakte The aim of the present investigation was to demonstrate an approach involving use of liquid chromatography (LC) and liquid chromatography-mass spectrometry (LC-MS) analytical techniques to separate, identify and characterize very small quantities of degradation products (DPs) of acebutolol without their isolation from the reaction mixtures. The drug was subjected to oxidative, hydrolytic, thermal and photolytic stress conditions as per International Confere...
Source: Journal of Pharmaceutical Analysis - March 16, 2018 Category: Drugs & Pharmacology Source Type: research

Whole body physiologically based modelling of β‐blockers in the rat: events in tissues and plasma following an i.v. bolus dose
Conclusions and ImplicationsPBPK modelling is a very powerful tool to aid drug discovery and development of therapeutic agents in animals and humans. However, careful consideration of the assumptions made during the modelling exercise is essential. (Source: British Journal of Pharmacology)
Source: British Journal of Pharmacology - December 1, 2017 Category: Drugs & Pharmacology Authors: S Y A Cheung, T Rodgers, L Aarons, I Gueorguieva, G L Dickinson, S Murby, C Brown, B Collins, M Rowland Tags: RESEARCH PAPER Source Type: research

Discovery of Potent Neuraminidase Inhibitors Using a Combination of Pharmacophore-Based Virtual Screening and Molecular Simulation Approach.
Abstract Neuraminidase (NA), a surface protein, facilitates the release of nascent virus and thus spreads infection. It has been renowned as a potential drug target for influenza A virus infection. The drugs such as oseltamivir, zanamivir, peramivir, and laninamivir are approved for the treatment of influenza infection. Additionally, investigational drugs namely MK2206, tamiphosphor, crenatoside, and dehydroepiandrosterone (DHEA) are also available for the treatment. However, recent outbreaks of highly pathogenic and drug-resistant influenza A strains highlighted the need to discover novel NA inhibitor. Keeping th...
Source: Applied Biochemistry and Biotechnology - October 23, 2017 Category: Biochemistry Authors: K R, V S Tags: Appl Biochem Biotechnol Source Type: research

Whole body physiologically based modelling of beta ‐blockers in the rat: Events in tissues and plasma following an intravenous bolus dose
Conclusions and ImplicationsPBPK modelling is a very powerful tool to aid drug discovery and development of therapeutic agents in animals and humans. However, careful consideration of the assumptions made during the modelling exercise is essential. (Source: British Journal of Pharmacology)
Source: British Journal of Pharmacology - October 20, 2017 Category: Drugs & Pharmacology Authors: S Y A Cheung, T Rodgers, L Aarons, I Gueorguieva, G L Dickinson, S Murby, C Brown, B Collins, M Rowland Tags: RESEARCH PAPER Source Type: research

Structural characterization of electrochemically and in vivo generated potential metabolites of selected cardiovascular drugs by EC-UHPLC/ESI-MS using an experimental design approach.
In this study, we employ a direct combination of electrochemical oxidation and mass spectrometric (EC-MS) identification for monitoring the oxidation pathway of ten cardiovascular drugs (metoprolol, propranolol, propafenone, mexiletine, oxprenolol, pirbuterol, pindolol, cicloprolol, acebutolol and atenolol). Oxidation was accomplished in an electrochemical thin-layer cell coupled on-line to electrospray ionization mass spectrometry (EC/ESI-MS). For further characterization of electrochemical products, the approach involving liquid chromatography linked to tandem mass spectrometry was used. Appropriate conditions for oxidat...
Source: Talanta - September 18, 2017 Category: Chemistry Authors: Szultka-Młyńska M, Bajkacz S, Baranowska I, Buszewski B Tags: Talanta Source Type: research

β1- and β2-adrenergic receptor stimulation differ in their effects on PGC-1α and atrogin-1/MAFbx gene expression in chick skeletal muscle
In this study, the effects of intraperitoneal injection of adrenaline and three β1–3-AR selective agonists on chick skeletal muscle metabolism were examined, to evaluate the functions of β-AR subtypes. Adrenaline decreased atrogin-1/MAFbx mRNA levels accompanied by an increase in PGC-1α mRNA and protein levels. However, among the three selective agonists, only the β1-AR agonist, dobutamine, increased PGC-1α mRNA and protein levels, while the β2-AR agonist, clenbuterol, suppressed atrogin-1/MAFbx mRNA levels. In addition, preinjection of the β1-AR antagonist, acebutolol, and the &b...
Source: Comparative Biochemistry and Physiology Part A: Molecular and Integrative Physiology - July 5, 2017 Category: Biochemistry Source Type: research

Mechanistic study of atenolol, acebutolol and carbamazepine adsorption on waste biomass derived activated carbon
Publication date: September 2017 Source:Journal of Molecular Liquids, Volume 241 Author(s): Ming-Ho To, Pejman Hadi, Chi-Wai Hui, Carol Sze Ki Lin, Gordon McKay Palm kernel shell (PKS) was physically activated by carbon dioxide at 900°C for 1.5h and tested for its ability to remove Atenolol (ATE), Acebutolol (ACE) and Carbamazepine (CBM), which are pharmaceutically active compounds (PhACs). Rapid adsorption of PhACs took place in the first 90min and reached equilibrium after 4h. The kinetic data were best fitted by the Ritchie-second-order model and confirmed by the diffusion-chemisorption model implying a predominant...
Source: Journal of Molecular Liquids - June 16, 2017 Category: Molecular Biology Source Type: research

β1- and β2-adrenergic receptor stimulation differ in their effects on PGC-1α and atrogin-1/MAFbx gene expression in chick skeletal muscle.
In this study, the effects of intraperitoneal injection of adrenaline and three β1-3-AR selective agonists on chick skeletal muscle metabolism were examined, to evaluate the functions of β-AR subtypes. Adrenaline decreased atrogin-1/MAFbx mRNA levels accompanied by an increase in PGC-1α mRNA and protein levels. However, among the three selective agonists, only the β1-AR agonist, dobutamine, increased PGC-1α mRNA and protein levels, while the β2-AR agonist, clenbuterol, suppressed atrogin-1/MAFbx mRNA levels. In addition, preinjection of the β1-AR antagonist, acebutolol, and the β2-...
Source: Comparative Biochemistry and Physiology. Part A, Molecular and integrative physiology. - May 31, 2017 Category: Physiology Authors: Shimamoto S, Ijiri D, Kawaguchi M, Nakashima K, Tada O, Inoue H, Ohtsuka A Tags: Comp Biochem Physiol A Mol Integr Physiol Source Type: research

Fast and sensitive analysis of beta blockers by ultra-highperformance liquid chromatography coupled with ultrahigh-resolution TOF mass spectrometry.
áclavík J Abstract This paper presents a method for the determination of acebutolol, betaxolol, bisoprolol, metoprolol, nebivolol and sotalol in human serum by liquid-liquid extraction (LLE) and ultra-high-performance liquid chromatography coupled with ultra-high-resolution TOF mass spectrometry (UHPLC-UHR-TOF MS). After liquid-liquid extraction, beta blockers were separated on a reverse phase analytical column Acclaim RS 120 (100 × 2.1 mm, 2.2 µm). The total run time was 6 min for each sample. Linearity, limit of detection (LOD), limit of quantification...
Source: Biomedical Chromatography : BMC - December 7, 2016 Category: Biomedical Science Authors: Tomková J, Ondra P, Kocianová E, Václavík J Tags: Biomed Chromatogr Source Type: research

Exploring the Feasibility of Biowaiver Extension of BCS Class III Drugs with Site-Specific Absorption Using Gastrointestinal Simulation Technology
Conclusions Based on the results of this study, we suggest that for BCS class III drug with high F a (about & gt;80  %), the biowaiver should extend to rapid dissolution ( T 85  %  = 30 min), and 30 % of F a as the boundary of intermediate permeability class (30  %  & lt;   F a   & lt;  85 %). (Source: European Journal of Drug Metabolism and Pharmacokinetics)
Source: European Journal of Drug Metabolism and Pharmacokinetics - July 22, 2016 Category: Drugs & Pharmacology Source Type: research

Synthesis and In Vitro Pharmacological Evaluation of 5 ‐(Alkoxymethyl)‐2‐(3‐alkylamino‐2‐hydroxypropoxy)phenylethanones Related to Acebutolol and Celiprolol
The structure–activity relationships of 13 analogs of aryloxyaminopropanol type derived from 2‐hydroxyphenylethanone as potential β‐blockers are described. The synthesized compounds possess an isopropyl or a tert‐butyl group in the hydrophilic part of the molecule and an alkoxymethyl substitution in the lipophilic moiety. The target compounds were prepared by an established four‐step method and their structures were confirmed by interpretation of their UV, IR, 1H NMR and 13C NMR spectra, and by elemental analysis. The β‐adrenolytic efficacy of the prepared racemic compounds was determined on isola...
Source: Archiv der Pharmazie - July 15, 2016 Category: Drugs & Pharmacology Authors: Katar ína Bruchatá, Andrej Némethy, Ružena Čižmáriková, Eva Račanská, Ladislav Habala Tags: Full Paper Source Type: research

Synthesis and In Vitro Pharmacological Evaluation of 5‐(Alkoxymethyl)‐2‐(3‐alkylamino‐2‐hydroxypropoxy)phenylethanones Related to Acebutolol and Celiprolol
The structure–activity relationships of 13 analogs of aryloxyaminopropanol type derived from 2‐hydroxyphenylethanone as potential β‐blockers are described. The synthesized compounds possess an isopropyl or a tert‐butyl group in the hydrophilic part of the molecule and an alkoxymethyl substitution in the lipophilic moiety. The target compounds were prepared by an established four‐step method and their structures were confirmed by interpretation of their UV, IR, 1H NMR and 13C NMR spectra, and by elemental analysis. The β‐adrenolytic efficacy of the prepared racemic compounds was determined on isola...
Source: Archiv der Pharmazie - July 1, 2016 Category: Drugs & Pharmacology Authors: Katarína Bruchatá, Andrej Némethy, Ružena Čižmáriková, Eva Račanská, Ladislav Habala Tags: Full Paper Source Type: research

Peripheral vasoconstriction induced by β‐adrenoceptor blockers: a systematic review and a network meta‐analysis
AimPeripheral vasoconstriction has long been described as a vascular adverse effect of β‐adrenoceptor blockers. Whether β‐adrenoceptor blockers should be avoided in patients with peripheral vascular disease depends on pharmacological properties (e.g. preferential binding to β1‐adrenoreceptors or intrinsic sympathomimetic activity). However, this has not been confirmed in experimental studies. We performed a network meta‐analysis in order to assess the comparative risk of peripheral vasoconstriction of different β‐adrenoceptor blockers. MethodWe searched for randomized controlled trials (R...
Source: British Journal of Clinical Pharmacology - May 31, 2016 Category: Drugs & Pharmacology Authors: Charles Khouri, Thomas Jouve, Sophie Blaise, Patrick Carpentier, Jean‐Luc Cracowski, Matthieu Roustit Tags: Meta ‐Analysis Source Type: research

Enantiomeric selectivity in adsorption of chiral β-blockers on sludge.
Enantiomeric selectivity in adsorption of chiral β-blockers on sludge. Environ Pollut. 2016 May 4;214:787-794 Authors: Sanganyado E, Fu Q, Gan J Abstract Adsorption of weakly basic compounds by sludge is poorly understood, although it has important implications on the distribution and fate of such micropollutants in wastewater effluent and sludge. Additionally, many of these compounds are chiral, and it is likely that their interactions with sludge is stereoselective and that the process may be further modified by surfactants that coexist in these systems. Adsorption of (R) and (S)-enantiomers of...
Source: Environmental Pollution - May 4, 2016 Category: Environmental Health Authors: Sanganyado E, Fu Q, Gan J Tags: Environ Pollut Source Type: research

Peripheral vasoconstriction induced by beta‐blockers: a systematic review and a network meta‐analysis.
Abstract AimPeripheral vasoconstriction has long been described as a vascular adverse effect of beta‐blockers. Whether beta‐blockers should be avoided in patients with peripheral vascular disease depends on pharmacological properties (e.g. preferential binding to β1‐adrenoreceptors or intrinsic sympathomimetic activity). However, this has not been confirmed in experimental studies. We performed a network meta‐analysis in order to assess the comparative risk of peripheral vasoconstriction of different beta‐blockers. MethodWe searched for randomized controlled trials (RCTs) including beta blockers that were pu...
Source: British Journal of Clinical Pharmacology - April 1, 2016 Category: Drugs & Pharmacology Authors: C. Khouri, T. Jouve, S. Blaise, P. Carpentier, J. L. Cracowski, M. Roustit Tags: Meta ‐analysis Source Type: research

Electrocatalytic redox behavior of graphene films towards acebutolol hydrochloride determination in real samples
New J. Chem., 2016, Advance ArticleDOI: 10.1039/C5NJ03655K, PaperAtmanand M. Bagoji, Sharanappa T. NandibewoorUnder optimal conditions, a graphene film modified glassy carbon electrode exhibited a longer linearity range from 3.36 to 57.12 ng mL-1 of acebutolol with a limit of detection of 0.131 ng mL-1.To cite this article before page numbers are assigned, use the DOI form of citation above.The content of this RSS Feed (c) The Royal Society of Chemistry (Source: RSC - New J. Chem. latest articles)
Source: RSC - New J. Chem. latest articles - March 4, 2016 Category: Chemistry Authors: Atmanand M. Bagoji Source Type: research

Electrocatalytic redox behavior of graphene film towards acebutolol hydrochloride determination in real samples
New J. Chem., 2016, Accepted ManuscriptDOI: 10.1039/C5NJ03655K, PaperAtmanand M Bagoji, Sharanappa T. NandibewoorThe electrochemical behavior of acebutolol (ACBT) at a thin graphene film modified glassy carbon electrode (GF-GCE) has been investigated using cyclic and differential pulse voltammetric techniques. An excellent electrocatalytic activity...The content of this RSS Feed (c) The Royal Society of Chemistry (Source: RSC - New J. Chem. latest articles)
Source: RSC - New J. Chem. latest articles - February 20, 2016 Category: Chemistry Authors: Atmanand M Bagoji Source Type: research

First Case Report of Smith–Magenis Syndrome (SMS) Among the Arab Community in Nazareth: View and Overview
This study comes to present a case of SMS in an Arab newborn male who was born in spontaneous delivery on June 29, 2015, with tachypnea, tracheomalacia, and mild hypotonia. The newborn was admitted on the Neonatal Intensive Care Unit (NICU), and various laboratory examinations and clinical examinations were performed. Throughout his hospitalization, feeding difficulties appeared and thus a peripheral venous catheter was inserted in the left leg. After 22 days of follow-up and hospitalizations, the patient status improved and he was discharged with recommendations to be in follow up in pediatric outpatient clinic. Howeve...
Source: Medicine - January 1, 2016 Category: Internal Medicine Tags: Research Article: Clinical Case Report Source Type: research

Aqueous chlorination of acebutolol: kinetics, transformation by-products, and mechanism.
This study investigated the reaction kinetics and the transformation by-products of acebutolol during aqueous chlorination. Acebutolol is one of the commonly used β-blockers for the treatment of cardiovascular diseases. It has been frequently detected in the aquatic environment. In the kinetics study, the second-order rate constant for the reaction between acebutolol and chlorine (k app) was determined at 25 ± 0.1 °C. The degradation of acebutolol by free available chlorine was highly pH dependence. When the pH increased from 6 to 8, it was found that the k app for the reaction between ac...
Source: Environmental Science and Pollution Research International - October 1, 2015 Category: Environmental Health Authors: Khalit WN, Tay KS Tags: Environ Sci Pollut Res Int Source Type: research

A proposed mechanism for the adverse effects of acebutolol: CES2 and CYP2C19-mediated metabolism and antinuclear antibody production.
Abstract Acebutolol, a β-adrenergic receptor-blocker, occasionally causes drug-induced lupus erythematosus (DILE). Acebutolol is mainly metabolized to diacetolol. Because metabolic activation has been considered to be related to acebutolol-induced toxicity, we sought to identify the enzymes that are responsible for acebutolol metabolism and investigate their involvement in acebutolol-induced toxicity. By using human liver microsomes (HLM) or intestinal microsomes and recombinant enzymes, we found that diacetolol was produced via hydrolysis by carboxylesterase 2 (CES2) and subsequent acetylation by N-acetyltra...
Source: Biochemical Pharmacology - September 22, 2015 Category: Drugs & Pharmacology Authors: Muta K, Fukami T, Nakajima M Tags: Biochem Pharmacol Source Type: research

Renewable sorbent material for solid phase extraction with direct coupling of sequential injection analysis-bead injection to liquid chromatography-electrospray ionization tandem mass spectrometry.
P, Smith N Abstract The use of small scale renewable sorbent material for automated solid phase extraction of multi-residue pharmaceuticals in environmental samples exploiting the sequential injection analysis-bead injection with direct coupling to liquid chromatography-electrospray ionization tandem mass spectrometry (SIA-BI-μSPE-LC-ESI-MS/MS) is presented to determine beta-blockers, namely atenolol, sotalol, pindolol, acebutolol, timolol, metoprolol, labetalol, carazolol, propranolol and betaxolol. These compounds yielded the same product ions, therefore were affected in terms of quantification when flo...
Source: Analytical and Bioanalytical Chemistry - May 14, 2015 Category: Chemistry Authors: Boonjob W, Sklenářová H, Barron L, Solich P, Smith N Tags: Anal Bioanal Chem Source Type: research

β-Blocker Dialyzability and Mortality in Older Patients Receiving Hemodialysis
This propensity-matched retrospective study showed that initiation of a high (atenolol, acebutolol, or metoprolol) versus low (bisoprolol or propranolol) -dialyzability β-blocker was associated with a higher risk of death in the following 180 days (relative risk, 1.4; 95% confidence interval, 1.1 to 1.8; P
Source: Nephrology Now - May 8, 2015 Category: Urology & Nephrology Authors: Nephrology Now editors Tags: Chronic Kidney Disease Clinical Nephrology Hemodialysis Source Type: research

{beta}-Blocker Dialyzability and Mortality in Older Patients Receiving Hemodialysis
Some β-blockers are efficiently removed from the circulation by hemodialysis ("high dialyzability") whereas others are not ("low dialyzability"). This characteristic may influence the effectiveness of the β-blockers among patients receiving long-term hemodialysis. To determine whether new use of a high-dialyzability β-blocker compared with a low-dialyzability β-blocker associates with a higher rate of mortality in patients older than age 66 years receiving long-term hemodialysis, we conducted a propensity-matched population-based retrospective cohort study using the linked healthcare...
Source: Journal of the American Society of Nephrology : JASN - March 31, 2015 Category: Urology & Nephrology Authors: Weir, M. A., Dixon, S. N., Fleet, J. L., Roberts, M. A., Hackam, D. G., Oliver, M. J., Suri, R. S., Quinn, R. R., Ozair, S., Beyea, M. M., Kitchlu, A., Garg, A. X. Tags: Clinical Research Source Type: research

Photocatalytic degradation of β-blockers by using immobilized titania/silica on glass slides
Publication date: Available online 3 March 2015 Source:Journal of Photochemistry and Photobiology A: Chemistry Author(s): Veronika Píšťková , Minoo Tasbihi , Milada Vávrová , Urška Lavrenčič Štangar Photocatalytic degradation of five β-blockers (acebutolol, atenolol, metoprolol, nadolol and propranolol) was investigated in aqueous media using immobilized TiO2 as a photocatalyst. The analyzed parameters were pharmaceutical removal and non purgable organic carbon. Two different types of photocatalyst incorporated in sol-gel matrix were compared; P25 exhibited a highe...
Source: Journal of Photochemistry and Photobiology A: Chemistry - March 5, 2015 Category: Chemistry Source Type: research

Comparative enantiomer affinity pattern of β‐blockers in aqueous and nonaqueous CE using single‐component anionic cyclodextrins
A series of eight chiral β‐blocker drugs, acebutolol, atenolol, carazolol, carteolol, carvedilol, propranolol, sotalol, and talinolol, have been enantioseparated using two single‐component anionic β‐CD derivatives, namely heptakis (2,3‐di‐O‐methyl‐6‐sulfo)‐β‐CD (HDMS‐β‐CD) and heptakis (2,3‐di‐O‐acetyl‐6‐sulfo)‐β‐CD (HDAS‐β‐CD), in aqueous CE and NACE. The influence of the nature of substituents (methyl or acetyl) in positions 2 and 3 on the CD derivatives and of the electrophoretic medium (water or methanol) on the enantioselectivity and enantiomer af...
Source: Electrophoresis - January 29, 2015 Category: Biochemistry Authors: Ying Feng, Tingting Wang, Zhengjin Jiang, Bezhan Chankvetadze, Jacques Crommen Tags: Research Article Source Type: research

Upregulation of P‐glycoprotein expression by ophthalmic drugs in different corneal in‐vitro models
ConclusionsThe expression and functionality of the P‐gp in corneal tissue can be influenced through time exposure with specific substrates. However, the exact mechanism still requires further elucidation. (Source: Journal of Pharmacy and Pharmacology)
Source: Journal of Pharmacy and Pharmacology - January 23, 2015 Category: Drugs & Pharmacology Authors: Jessica Verstraelen, Stephan Reichl Tags: Research Paper Source Type: research

Blood pressure lowering efficacy of partial agonist beta blocker monotherapy for primary hypertension.
CONCLUSIONS: There was very low quality evidence that in patients with moderate to severe hypertension, partial agonists lowered peak BP by an average of 8/4 mmHg and reduced heart rate by five beats per minute. There was no evidence of a greater effect at doses higher than the initial doses. This estimate was probably exaggerated as it was subject to a high risk of bias. Based on the indirect comparison of the results in this review and two Cochrane reviews on angiotensin-converting-enzyme (ACE) inhibitors and angiotensin receptor blockers (ARBs), which also used similar inclusion criteria as this review, the BP lowering ...
Source: Cochrane Database of Systematic Reviews - December 2, 2014 Category: Journals (General) Authors: Wong GW, Boyda HN, Wright JM Tags: Cochrane Database Syst Rev Source Type: research

Comparative enantiomer affinity pattern of β‐blockers in aqueous and non‐aqueous CE using single‐component anionic cyclodextrins
This article is protected by copyright. All rights reserved (Source: Electrophoresis)
Source: Electrophoresis - November 1, 2014 Category: Biochemistry Authors: Ying Feng, Tinting Wang, Zhengjin Jiang, Bezhan Chankvetadze, Jacques Crommen Tags: Research Paper Source Type: research

Retention and selectivity of basic drugs on solid-phase extraction sorbents: Application to direct determination of β-blockers in urine.
Retention and selectivity of basic drugs on solid-phase extraction sorbents: Application to direct determination of β-blockers in urine. Anal Bioanal Chem. 2014 May 2; Authors: Boonjob W, Sklenářová H, Lara FJ, García-Campaña AM, Solich P Abstract Seven solid phase sorbent materials with reversed-phase, mixed-mode interactions (ion-exchange and reversed-phase), and molecularly imprinted polymers (MIP), namely Oasis HLB, Oasis MAX, Oasis MCX, Bond Elute Plexa, Bond Elute Plexa PAX, Bond Elute Plexa PCX, and SupelMIP sorbents, were investigated. The present study was fo...
Source: Analytical and Bioanalytical Chemistry - May 2, 2014 Category: Chemistry Authors: Boonjob W, Sklenářová H, Lara FJ, García-Campaña AM, Solich P Tags: Anal Bioanal Chem Source Type: research

Interactions of beta-blockers with model lipid membranes Molecular view of the interaction of acebutolol, oxprenolol, and propranolol with phosphatidylcholine vesicles by time-dependent fluorescence shift and molecular dynamics simulations.
f M Abstract Since pharmacokinetic and pharmacodynamic activities of drugs are often related to their interactions with biomembranes, it is of high interest to establish an approach for the characterization of these interactions at the molecular level. For the present study beta-blockers (oxprenolol, propranolol, and acebutolol) were selected due to their well described nonspecific membrane effects (NME). Their interactions with model lipid membranes composed of palmitoyloleoylphosphatidylcholine (POPC) were studied using Time-Dependent Fluorescence Shift (TDFS) and Generalized Polarization (GP) as well as molecul...
Source: European Journal of Pharmaceutics and Biopharmaceutics - March 27, 2014 Category: Drugs & Pharmacology Authors: Först G, Cwiklik L, Jurkiewicz P, Schubert R, Hof M Tags: Eur J Pharm Biopharm Source Type: research

Impact of wastewater treatment plants on receiving surface waters and a tentative risk evaluation: the case of estrogens and beta blockers.
ery M Abstract Five estrogenic hormones (unconjugated + conjugated fractions) and 10 beta blockers were analyzed in three wastewater treatment plant (WWTP) effluents and receiving river waters in the area of Lyon, France. In the different samples, only two estrogens were quantified: estrone and estriol. Some beta blockers, such as atenolol, acebutolol, and sotalol, were almost always quantified, but others, e.g., betaxolol, nadolol, and oxprenolol were rarely quantified. Concentrations measured in river waters were in the nanogram per liter range for estrogens and between 0.3 and 210 ng/L for be...
Source: Environmental Science and Pollution Research International - August 24, 2013 Category: Environmental Health Authors: Gabet-Giraud V, Miège C, Jacquet R, Coquery M Tags: Environ Sci Pollut Res Int Source Type: research