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Chemosphere Jan 2022Acebutolol (ACE) has been widely used for the treatment of cardiovascular disorders, and its photochemical fate in natural waters is a matter of concern due to its...
Acebutolol (ACE) has been widely used for the treatment of cardiovascular disorders, and its photochemical fate in natural waters is a matter of concern due to its ubiquitous occurrence and its toxicity to aquatic organisms. In this study, the photodegradation of ACE in river water and synthetic waters were investigated under simulated sunlight irradiation. The results demonstrated that ACE photodegradation rate in river water was 3.2 times higher than that in pure water. Then the influences of HCO, NO and DOM on ACE photolysis were investigated under their concentrations similar with the ones in river water. ACE photodegradation was significantly enhanced in the presence of HCO alone, and the scavenging experiments and the electron paramagnetic resonance experiments together proved that HCO could be oxidized by triplet-excited state of ACE to generate CO, which subsequently played a key role in ACE degradation. The presence of both NO and DOM also increased the ACE photodegradation rates, and •OH and DOM* were found to be involved in the degradation. In addition, when DOM was added to a solution with HCO, the enhancement effect of HCO on ACE photodegradation was weakened due to the scavenging of CO by DOM combined with the light screening effect of DOM.
Topics: Acebutolol; Carbonates; Hydroxyl Radical; Photolysis; Water Pollutants, Chemical
PubMed: 34826949
DOI: 10.1016/j.chemosphere.2021.132318 -
Journal of Hazardous Materials Feb 2022The excessive cost, unsustainability or complex production of new highly selective electrocatalysts for HO production, especially noble-metal-based ones, is prohibitive...
The excessive cost, unsustainability or complex production of new highly selective electrocatalysts for HO production, especially noble-metal-based ones, is prohibitive in the water treatment sector. To solve this conundrum, biomass-derived carbons with adequate textural properties were synthesized via agarose double-step pyrolysis followed by steam activation. A longer steam treatment enhanced the graphitization and porosity, even surpassing commercial carbon black. Steam treatment for 20 min yielded the greatest surface area (1248 m g), enhanced the mesopore/micropore volume distribution and increased the activity (E = 0.609 V) and yield of HO (40%) as determined by RRDE. The upgraded textural properties had very positive impact on the ability of the corresponding gas-diffusion electrodes (GDEs) to accumulate HO, reaching Faradaic current efficiencies of ~95% at 30 min. Acidic solutions of β-blocker acebutolol were treated by photoelectro-Fenton (PEF) process in synthetic media with and without chloride. In urban wastewater, total drug disappearance was reached at 60 min with almost 50% mineralization after 360 min at only 10 mA cm. Up to 14 degradation products were identified in the Cl-containing medium.
Topics: Acebutolol; Chlorides; Electrodes; Hydrogen Peroxide; Iron; Oxidation-Reduction; Sepharose; Water Pollutants, Chemical
PubMed: 34479080
DOI: 10.1016/j.jhazmat.2021.127005 -
Current Drug Metabolism 2021Adrenergic β-blockers are used to treat many conditions, including hypertension, cardiac arrhythmias, heart failure, angina pectoris, migraine, and tremors. The... (Review)
Review
Adrenergic β-blockers are used to treat many conditions, including hypertension, cardiac arrhythmias, heart failure, angina pectoris, migraine, and tremors. The majority of the β-blockers including Propranolol, Metoprolol, Acebutolol, Alprenolol, Betaxolol, Carvedilol, Nebivolol and Oxprenolol are metabolised majorly by CYP2D6, and Bisoprolol is primarily metabolised by CYP3A4 enzymes. The drugs inhibiting or inducing them may alter the pharmacokinetics of those β-blockers. The plasma concentrations of Propranolol might be elevated by the concomitant use of drugs, such as SSRIs (Fluoxetine, Paroxetine), SNRIs (Duloxetine) and Cimetidine, while the plasma concentrations of Metoprolol increased by the concurrent use of SSRIs (Fluoxetine, Paroxetine), Amiodarone, Celecoxib, Cimetidine, Terbinafine, and Diphenhydramine. β-blockers can also interact pharmacodynamically with drugs, including fluoroquinolones, antidiabetic agents and NSAIDs. In addition, β-blockers may interact with herbs, such as curcumin, Ginkgo biloba, Schisandra chinensis, green tea, guggul, hawthorn, St. John's wort and Yohimbine. This article focuses on clinically relevant drug interactions of β-blockers with commonly prescribed medications. In addition to Pharmacokinetics and Pharmacodynamics of the drug interactions, recommendations for clinical practice are highlighted. The prescribers and the pharmacists are needed to be aware of the drugs interacting with β-blockers to prevent possible adverse drug interactions.
Topics: Adrenergic beta-Antagonists; Drug Interactions; Humans; Medication Therapy Management; Pharmaceutical Preparations
PubMed: 34182907
DOI: 10.2174/1389200222666210614112529 -
Critical Care (London, England) Jun 2021β-adrenergic antagonists (BAAs) are used to treat cardiovascular disease such as ischemic heart disease, congestive heart failure, dysrhythmias, and hypertension....
BACKGROUND
β-adrenergic antagonists (BAAs) are used to treat cardiovascular disease such as ischemic heart disease, congestive heart failure, dysrhythmias, and hypertension. Poisoning from BAAs can lead to severe morbidity and mortality. We aimed to determine the utility of extracorporeal treatments (ECTRs) in BAAs poisoning.
METHODS
We conducted systematic reviews of the literature, screened studies, extracted data, and summarized findings following published EXTRIP methods.
RESULTS
A total of 76 studies (4 in vitro and 2 animal experiments, 1 pharmacokinetic simulation study, 37 pharmacokinetic studies on patients with end-stage kidney disease, and 32 case reports or case series) met inclusion criteria. Toxicokinetic or pharmacokinetic data were available on 334 patients (including 73 for atenolol, 54 for propranolol, and 17 for sotalol). For intermittent hemodialysis, atenolol, nadolol, practolol, and sotalol were assessed as dialyzable; acebutolol, bisoprolol, and metipranolol were assessed as moderately dialyzable; metoprolol and talinolol were considered slightly dialyzable; and betaxolol, carvedilol, labetalol, mepindolol, propranolol, and timolol were considered not dialyzable. Data were available for clinical analysis on 37 BAA poisoned patients (including 9 patients for atenolol, 9 for propranolol, and 9 for sotalol), and no reliable comparison between the ECTR cohort and historical controls treated with standard care alone could be performed. The EXTRIP workgroup recommends against using ECTR for patients severely poisoned with propranolol (strong recommendation, very low quality evidence). The workgroup offered no recommendation for ECTR in patients severely poisoned with atenolol or sotalol because of apparent balance of risks and benefits, except for impaired kidney function in which ECTR is suggested (weak recommendation, very low quality of evidence). Indications for ECTR in patients with impaired kidney function include refractory bradycardia and hypotension for atenolol or sotalol poisoning, and recurrent torsade de pointes for sotalol. Although other BAAs were considered dialyzable, clinical data were too limited to develop recommendations.
CONCLUSIONS
BAAs have different properties affecting their removal by ECTR. The EXTRIP workgroup assessed propranolol as non-dialyzable. Atenolol and sotalol were assessed as dialyzable in patients with kidney impairment, and the workgroup suggests ECTR in patients severely poisoned with these drugs when aforementioned indications are present.
Topics: Adrenergic beta-Antagonists; Consensus; Drug Overdose; Extracorporeal Membrane Oxygenation; Humans
PubMed: 34112223
DOI: 10.1186/s13054-021-03585-7 -
Annales Pharmaceutiques Francaises Sep 2021The aim of this study was to predict the plasma concentrations of acebutolol tablets with different dissolution profiles using computer modelling and evaluating whether...
PURPOSE
The aim of this study was to predict the plasma concentrations of acebutolol tablets with different dissolution profiles using computer modelling and evaluating whether they are bioequivalent using simulated population studies.
METHODS
The dissolution behaviour of acebutolol was studied in the USP Apparatus-II using different dissolution media for pH 1.2, 4.5, and 6.8 at 37±0.5°C. The obtained dissolution data, as well as plasma concentration-time data of the reference product from the literature were used as inputs to build pharmacokinetic model of acebutolol within GastroPlus™ software (version 9.7, Simulations Plus Inc., Lancaster, CA, USA) to simulate the in vivo profiles of the drug.
RESULTS
The dissolution profiles of the reference product Sectral® 400mg tablets and a locally produced generic product were>85% in 15min in three dissolution media. Simulation results demonstrated that the brand and generic products would show the same in vivo performance. Population simulation results of the ln-transformed 90% confidence interval for the ratio of C, AUC and AUC values for the two products were within the 80-125% interval, showing to be bioequivalent.
CONCLUSION
Based on the in vitro results combined with in silico simulations using GastroPlus™, a biowaiver for immediate release acebutolol tablets is justified. Furthermore, computer modelling has shown to be a very intersting tool to prove the bioequivalence for these products.
Topics: Acebutolol; Computer Simulation; Solubility; Tablets; Therapeutic Equivalency
PubMed: 33675740
DOI: 10.1016/j.pharma.2021.02.004 -
Mikrochimica Acta Mar 2021Molybdenum disulfide (MoS) surface functionalization was performed with a catechol-containing polymer sodium alginate (SA) and dopamine (DA) through simultaneous MoS...
Molybdenum disulfide (MoS) surface functionalization was performed with a catechol-containing polymer sodium alginate (SA) and dopamine (DA) through simultaneous MoS exfoliation and self-polymerization of DA. The MoS/SA-PDA nanocomposite was characterized using spectroscopic, microscopic, and electroanalytical techniques to evaluate its electrocatalytic performance. The electrocatalytic behavior of the MoS/SA-PDA nanocomposite modified electrode for the detection of acebutolol (ACE), a cardio-selective β-blocker drug was explored through cyclic voltammetric and differential pulse voltammetric techniques. The influence of scan rate, concentration, and pH value on the oxidation peak current of ACE was investigated to optimize the deducting condition. The electrochemical activity of the MoS/SA-PDA nanocomposite electrode was attributed to the existence of reactive functional groups being contributed from SA, PDA, and MoS exhibiting a synergic effect. The MoS/SA-PDA nanocomposite modified electrode exhibits admirable electrocatalytic activity with a wide linear response range (0.009 to 520 μM), low detection limit (5 nM), and high sensitivity (0.354 μA μM cm) also in the presence of similar (potentially interfering) compounds. The fabricated MoS/SA-PDA nanocomposite modified electrode can be useful for the detection of ACE in pharmaceutical analysis.
Topics: Acebutolol; Adrenergic beta-1 Receptor Antagonists; Alginates; Biosensing Techniques; Disulfides; Electrochemical Techniques; Electrodes; Humans; Indoles; Limit of Detection; Molybdenum; Nanocomposites; Oxidation-Reduction; Polymers; Reproducibility of Results
PubMed: 33646401
DOI: 10.1007/s00604-021-04717-0 -
Journal of Colloid and Interface Science May 2021The novel environment-friendly hexadecanoamide propyltrimethy lammonium chloride (NQAS16-3) surfactant with different amounts (0.2, 0.4, 0.6, 0.8, 1.0, 1.2 CEC) was...
Adsorption of two β-blocker pollutants on modified montmorillonite with environment-friendly cationic surfactant containing amide group: Batch adsorption experiments and Multiwfn wave function analysis.
The novel environment-friendly hexadecanoamide propyltrimethy lammonium chloride (NQAS16-3) surfactant with different amounts (0.2, 0.4, 0.6, 0.8, 1.0, 1.2 CEC) was firstly used to modify montmorillonite, and the obtained organomontmorillonite (N-Mt) with the amount of surfactant equal to 1.0 CEC was utilized to adsorb two β-blocker pollutants- Atenolol (ATE) and acebutolol (ACE). The experimental results indicated that the equilibrium adsorption capacity of N-Mt(the organo-montmorillonite that the amount of modifier was 1.0 CEC) for ATE and ACE was 93.47 mg/g and 84.55 mg/g, respectively, which was more than twice that of raw montmorillonite for two pollutants, the adsorption was better fitted with the pseudo-second-order model and Langmuir isotherms model, and the adsorption was the spontaneous and exothermic process. Moreover, combining with the Zeta potential values of N-Mt, and with the help of Multiwfn wave function program based on density functional theory (DFT), the electrostatic interaction and the hydrophobic partitioning between N-Mt and two pollutant molecules were verified, p-π/π interaction between NQAS16-3 and ATE (or ACE) may be contributed to the increasing adsorption capacity of N-Mt for two β-blocker pollutants. The work provided novel organomontmorillonite for the removal of non-degradable β-blocker pollutants and the insight of the adsorption mechanism from the atomic level.
PubMed: 33582363
DOI: 10.1016/j.jcis.2021.01.077 -
Ecotoxicology and Environmental Safety Apr 2021MoS/montmorillonite (MoS/Mt) composite was successfully synthesized through a simple hydrothermal method, and its adsorption performance for two emerging...
The adsorption performance and micro-mechanism of MoS/montmorillonite composite to atenolol and acebutolol: Adsorption experiments and a novel visual study of interaction.
MoS/montmorillonite (MoS/Mt) composite was successfully synthesized through a simple hydrothermal method, and its adsorption performance for two emerging contaminants-atenolol (ATE) and acebutolol (ACE) was researched. The batch experiments revealed that the adsorption process can be described by the Pseudo-second order model and Langmuir model, and the adsorption capacity of MoS/Mt, MoS and Mt for ATE were 132.08 mg/g, 60.68 mg/g and 74.23 mg/g, for ACE were 113.82 mg/g, 33.01 mg/g and 36.05 mg/g, respectively. Besides, Fourier-transform infrared spectroscopy (FTIR), BET specific surface area measurement and X-ray photoelectron spectroscopy (XPS) were also employed to analyze the adsorption mechanism. Moreover, quantitative molecular surface analysis and weak intermolecular interaction analysis with independent gradient model were combined to probe the microscopic interaction between the adsorbent and adsorbate. The results indicated the interactions included hydrogen bonding and vdW interaction. Mt and MoS interacted more strongly with ATE than ACE, which revealed the reason MoS/Mt, Mt and MoS possessed higher adsorption capacity for ATE.
Topics: Acebutolol; Adsorption; Atenolol; Bentonite; Hydrogen Bonding; Hydrogen-Ion Concentration; Kinetics; Molybdenum; Photoelectron Spectroscopy; Spectroscopy, Fourier Transform Infrared; Water Pollutants, Chemical
PubMed: 33578102
DOI: 10.1016/j.ecoenv.2021.111993 -
Turkish Journal of Pharmaceutical... Dec 2020Acebutolol HCl (ABL) is a selective β-adrenergic receptor blocking agent that is preferably administered by the oral route despite its low bioavailability (30-50%). The...
OBJECTIVES
Acebutolol HCl (ABL) is a selective β-adrenergic receptor blocking agent that is preferably administered by the oral route despite its low bioavailability (30-50%). The purpose of this study was to evaluate the effect of verapamil HCl (VER) [as P-glycoprotein inhibitor (P-gp)] on the intestinal absorption of ABL by comparing the changes in the absorption rate constant (k) of ABL.
MATERIALS AND METHODS
intestinal perfusion was conducted in healthy male Wistar albino rats to study the absorption phase of ABL. Eighteen rats were divided into three groups. The first group (the control group) was perfused with ABL alone (260 μg/mL). The second and third groups were perfused with ABL (260 μg/mL) in combination with VER at different concentrations (200 and 400 μg/mL, respectively). The analysis was performed using a simple, rapid, and validated spectroscopic method.
RESULTS
The absorption study showed that k of ABL in the first group was 0.47±0.045 h-. In the third group k increased 3-fold (1.37±0.031 h-); however, the second group showed a statistically insignificant change in k (0.39±0.076 h-).
CONCLUSION
The results revealed that VER at a concentration of 400 μg/mL has a pronounced effect on the absorption kinetics of ABL (increased k). This could be linked to the inhibition of P-gp, which is considered a contributing factor in low bioavailability of ABL.
PubMed: 33389978
DOI: 10.4274/tjps.galenos.2019.59862 -
Molecules (Basel, Switzerland) Nov 2020In this work, one of the most prevalent polypharmacology drug-drug interaction events that occurs between two widely used beta-blocker drugs-i.e., acebutolol and...
In this work, one of the most prevalent polypharmacology drug-drug interaction events that occurs between two widely used beta-blocker drugs-i.e., acebutolol and propranolol-with the most abundant blood plasma fibrinogen protein was evaluated. Towards that end, molecular docking and Density Functional Theory (DFT) calculations were used as complementary tools. A fibrinogen crystallographic validation for the three best ranked binding-sites shows 100% of conformationally favored residues with total absence of restricted flexibility. From those three sites, results on both the binding-site druggability and ligand transport analysis-based free energy trajectories pointed out the most preferred biophysical environment site for drug-drug interactions. Furthermore, the total affinity for the stabilization of the drug-drug complexes was mostly influenced by steric energy contributions, based mainly on multiple hydrophobic contacts with critical residues (THR22: P and SER50: Q) in such best-ranked site. Additionally, the DFT calculations revealed that the beta-blocker drug-drug complexes have a spontaneous thermodynamic stabilization following the same affinity order obtained in the docking simulations, without covalent-bond formation between both interacting beta-blockers in the best-ranked site. Lastly, experimental ultrasound density and velocity measurements were performed and allowed us to validate and corroborate the computational obtained results.
Topics: Adrenergic beta-Antagonists; Binding Sites; Density Functional Theory; Drug Interactions; Fibrinogen; Ligands; Molecular Conformation; Molecular Docking Simulation; Reproducibility of Results; Thermodynamics
PubMed: 33228181
DOI: 10.3390/molecules25225425