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Molecules (Basel, Switzerland) Jun 2024Atenolol (ATE) and propranolol (PRO) inclusion complexes with β-cyclodextrin have been investigated in aqueous solution. The aqueous solution was examined and...
Atenolol (ATE) and propranolol (PRO) inclusion complexes with β-cyclodextrin have been investigated in aqueous solution. The aqueous solution was examined and characterized using UV-vis, fluorescence spectroscopy, and H NMR. The physical mixture was characterized using FTIR. The existence of inclusion complexes is confirmed by observing changes in spectroscopic properties. The ATE complex with β-CD exhibited an interaction as host and (β-CD) as a guest in a 1:1 ratio, with an inclusion constant K of 2.09 × 10 µM, as determined by the typical double-reciprocal graphs. Similarly, the PRO complex with β-CD exhibited an interaction as host and (β-CD) guest in 1:1 and 1:2 stoichiometry at the same time; the inclusion constants were K1 = 5.80 × 10 µM and K2 = 4.67 × 10 µM, as determined by typical double-reciprocal graphs. The variables influencing the formation of the inclusion complexes were investigated and optimized. Based on the enhancement in fluorescence intensity due to the formation of inclusion complexes, spectrofluorometric methods were developed and validated for determination of each drug's pharmaceutical formulation. The quantification of the fluorescence intensity for ATE and PRO was conducted at λ/λ 226/302 nm and λ/λ 231/338 nm, respectively. Under the optimal reaction circumstances, linear relationships with good correlation coefficients of 0.9918 and 0.99 were found in the concentration ranges of 0.3-1.7 μM, and 0.1-1.1 μM for ATE and PRO, respectively. The limits of detection (LODs) were found to be 0.13 and 0.01 μM for ATE and PRO, respectively. The suggested approach was effectively applied to the analysis of both drugs' pharmaceutical formulations.
Topics: Atenolol; beta-Cyclodextrins; Propranolol; Spectrometry, Fluorescence; Spectroscopy, Fourier Transform Infrared; Magnetic Resonance Spectroscopy
PubMed: 38930938
DOI: 10.3390/molecules29122875 -
Chemosphere Aug 2022Biodegradation is regarding as the most important organic micro-pollutants (OMPs) removal mechanism during riverbank filtration (RBF), but the OMPs co-metabolism...
Biodegradation is regarding as the most important organic micro-pollutants (OMPs) removal mechanism during riverbank filtration (RBF), but the OMPs co-metabolism mechanism and the role of NH-N during this process are not well understood. Here, we selected atenolol as a typical OMP to explore the effect of NH-N concentration on atenolol removal and the role of ammonia oxidizing bacteria (AOB) in atenolol biodegradation. The results showed that RBF is an effective barrier for atenolol mainly by biodegradation and adsorption. The ratio of biodegradation and adsorption to atenolol removal was dependent on atenolol concentration. Specifically, atenolol with low concentration (500 ng/L) is almost completely removed by adsorption, while atenolol with higher concentration (100 μg/L) is removed by biodegradation (51.7%) and adsorption (30.8%). Long-term difference in influent NH-N concentrations did not show significant impact on atenolol (500 ng/L) removal, which was mainly dominated by adsorption. Besides, AOB enhanced the removal of atenolol (100 μg/L) as biodegradation played a more crucial role in removing atenolol under this concentration. Both AOB and heterotrophic bacteria can degrade atenolol during RBF, but the degree of AOB's contribution may be related to the concentration of atenolol exposure. The main reactions occurred during atenolol biodegradation possibly includes primary amide hydrolysis, hydroxylation and secondary amine depropylation. About 90% of the bio-transformed atenolol was produced as atenolol acid. AOB could transform atenolol to atenolol acid by inducing primary amide hydrolysis but failed to degrade atenolol acid further under the conditions of this paper. This study provides novel insights regarding the roles played by AOB in OMPs biotransformation during RBF.
Topics: Amides; Ammonia; Atenolol; Betaproteobacteria; Biodegradation, Environmental; Filtration; Oxidation-Reduction
PubMed: 35447203
DOI: 10.1016/j.chemosphere.2022.134653 -
Pakistan Journal of Pharmaceutical... Mar 2016Objective of this study is to develop; tablet-in-a capsule system, to deliver Atenolol 25mg and Glyburide 5mg in the hard gelatin capsule. In order to improve patient... (Comparative Study)
Comparative Study
PURPOSE
Objective of this study is to develop; tablet-in-a capsule system, to deliver Atenolol 25mg and Glyburide 5mg in the hard gelatin capsule. In order to improve patient compliance and reduce problems associated with complex therapeutic regimen Atenolol (cardio-selective beta-blocker) and Glyburide (anti-diabetic; sulfonylurea) are commonly, prescribed to the diabetic hypertensive patient. Metgod: In present work six different formulations of Atenolol (AF1-AF6) and Glyburide (GF1-GF6) were prepared by direct compression method using Avicel, Lactose DC, Crospovidone and Magnesium Stearate in different proportions and encapsulated in hard gelatin shells. Post compression parameters i.e. weight variation, diameter variation, thickness variation, hardness variation, % friability, disintegration, % drug release were determined at different pH 1.2, 4.5 and 6.8, and subjected to dissolution profile comparison through similarity factor (ƒ2).
RESULTS
Stability studies were performed and shelf lives were calculated by R-Gui Stab R console 2.15.2 and determined to be 15 and 27 months for Atenolol and Glyburide respectively. The percentage drug contents of Atenolol and Glyburide were estimated spectrophotometerically at 286 nm and 314.7 nm respectively. Formulations CF1-CF6 (encapsulated) were subjected to weight variation, disintegration and dissolution tests and subjected to model dependant analysis for dissolution studies. The simultaneous quantitation of Atenolol and Glyburide for content assay was done by HPLC method of analysis.
CONCLUSION
formulation CF6 is showing highest coefficient of correlation values for all models applied. So we can conclude that the proposed system can improve patient compliance by increasing the ease of administration of two drugs together.
Topics: Administration, Oral; Adrenergic beta-1 Receptor Antagonists; Atenolol; Capsules; Chemistry, Pharmaceutical; Chromatography, High Pressure Liquid; Diffusion; Drug Combinations; Drug Stability; Excipients; Glyburide; Hardness; Hydrogen-Ion Concentration; Hypoglycemic Agents; Kinetics; Models, Chemical; Solubility; Spectrophotometry, Ultraviolet; Tablets; Technology, Pharmaceutical
PubMed: 27087100
DOI: No ID Found -
Medwave Dec 2023Infantile hemangioma is the most frequent benign vascular tumor in childhood, with an incidence of 3 to 10%. When patients require treatment, oral propranolol, a... (Meta-Analysis)
Meta-Analysis
INTRODUCTION
Infantile hemangioma is the most frequent benign vascular tumor in childhood, with an incidence of 3 to 10%. When patients require treatment, oral propranolol, a non-selective lipophilic beta-blocker, is usually considered the therapy of choice. However, its use has been associated with several adverse events related to its β-2 action and its ability to cross the blood-brain barrier. Because of this, oral atenolol, a hydrophilic β-1 receptor-selective beta-blocker, may represent a valid treatment alternative. Nonetheless, there is still controversy regarding the efficacy and safety of atenolol when compared with propranolol as monotherapy for this condition.
METHODS
We searched Epistemonikos, the largest database of systematic reviews in health science, which is maintained by screening multiple sources of information, including MEDLINE/PubMed, EMBASE, and Cochrane, among others. Data were extracted from the identified reviews, data from the primary studies were analyzed, a meta-analysis was performed, and a summary table of the results was prepared using the Grading of Recommendations Assessment, Development, and Evaluation (GRADE) method.
RESULTS
Nine systematic reviews were identified, including 10 primary studies and three randomized trials. The three randomized trials were included in the analysis of this investigation.
CONCLUSION
The use of oral atenolol compared with oral propranolol as monotherapies may result in little or no difference in terms of likelihood of complete remission, decrease in Hemangioma Activity Score, likelihood of post-treatment relapse, and risk of adverse events and severe adverse events, in infantile hemangioma (low certainty of evidence).
Topics: Humans; Propranolol; Atenolol; Treatment Outcome; Neoplasm Recurrence, Local; Systematic Reviews as Topic; Adrenergic beta-Antagonists; Hemangioma, Capillary; Hemangioma
PubMed: 38061014
DOI: 10.5867/medwave.2023.11.2753 -
Environmental Pollution (Barking, Essex... Apr 2022The beta-blocker atenolol (ATE), and the selective serotonin and norepinephrine reuptake inhibitor, venlafaxine (VEN) are frequently detected in municipal wastewater...
The beta-blocker atenolol (ATE), and the selective serotonin and norepinephrine reuptake inhibitor, venlafaxine (VEN) are frequently detected in municipal wastewater effluents, but little is known about their ecotoxicological effect on aquatic animals. Herein, ATE and VEN were selected to explore their accumulation and global DNA methylation (GDM) in zebrafish tissues after a 30-day exposure. Molecular dynamics (MD) stimulation was used to investigate the toxic mechanism of ATE and VEN exposure. The results demonstrated that ATE and VEN could reduce the condition factor of zebrafish. The bioaccumulation capacity for ATE and VEN was in the order of liver > gut > gill > brain and liver > gut > brain > gill, respectively. After a 30-day recovery, ATE and VEN could still be detected in zebrafish tissues when exposure concentrations were ≥10 μg/L. Moreover, ATE and VEN induced global DNA hypomethylation in different tissues with a dose-dependent manner and their main target tissues were liver and brain. When the exposure concentrations of ATE and VEN were increased to 100 μg/L, the global DNA hypomethylation of liver and brain were reduced to 27% and 18%, respectively. In the same tissue exposed to the same concentration, DNA hypomethylation induced by VEN was more serious than that of ATE. After a 30-day recovery, the global DNA hypomethylations caused by the two drugs were still persistent, and the recovery of VEN was slower than that of ATE. The MD simulation results showed that both ATE and VEN could reduce the catalytic activity of DNA Methyltransferase 1 (DNMT1), while the effect of VEN on the 3D conformational changes of the DNMT1 domain was more significant, resulting in a lower DNA methylation rate. The current study shed new light on the toxic mechanism and potential adverse impacts of ATE and VEN on zebrafish, providing essential information to the further ecotoxicological risk assessment of these drugs in the aquatic environment.
Topics: Animals; Atenolol; Bioaccumulation; DNA; DNA Methylation; Venlafaxine Hydrochloride; Zebrafish
PubMed: 35081461
DOI: 10.1016/j.envpol.2022.118898 -
Chirality Jun 2022Chiral separation of β-blockers is performed by utilizing the supercritical fluid chromatographic method. The chiral columns utilized were Chiralpak IG and Chiralpak... (Review)
Review
Chiral separation of β-blockers is performed by utilizing the supercritical fluid chromatographic method. The chiral columns utilized were Chiralpak IG and Chiralpak IBN-5. The finest mobile phase was CO -0.2% TEA in methanol (60:40). The values atenolol enantiomers retention factors were 6.39 and 8.98. These values for propranolol enantiomers were 3.39 and 4.06. These values for betaxolol enantiomers were 4.08 and 4.68. The separation and resolution factor values for atenolol, propranolol, and betaxolol were 1.41 and 3.33, 1.19 and 2.23, and 1.15 and 1.87, separately and respectively. By comparison, it was observed that Chiralpak IG column is better than Chiralpak IBN-5 column. Supercritical fluid chromatography has been found as the best analytical technique due to its high speed, being eco-friendly, and being economic. The various most probable interactions responsible for the chiral resolution are hydrogen bonding, dipole-dipole interactions, steric effect, and π-π interactions. The reported methods are effective, efficient, and reproducible and may be used to separate and identify atenolol, propranolol, and betaxolol in any unknown samples.
Topics: Adrenergic beta-Antagonists; Atenolol; Betaxolol; Chromatography, Supercritical Fluid; Propranolol; Stereoisomerism
PubMed: 35297109
DOI: 10.1002/chir.23440 -
European Journal of Pediatrics Feb 2023The purpose of this study was to compare long-term neurocognitive functioning (working memory, processing speed, and attention) between children who had been treated...
UNLABELLED
The purpose of this study was to compare long-term neurocognitive functioning (working memory, processing speed, and attention) between children who had been treated with either propranolol or atenolol for infantile hemangioma during infancy. All eligible children (n = 158) aged 6 years or older and treated with propranolol or atenolol as infants were invited to participate in this two-center cross-sectional study. The primary outcome was the Wechsler Intelligence Scale for Children-V Cognitive Proficiency Index (CPI), a measure of working memory, processing speed, and attention. Secondary outcomes were general intelligence, auditory, visuospatial, and narrative memory, as well as executive functioning and sleep. A total of 105 children, of whom 36 had been treated with propranolol (age 6.0-11.8 years, follow-up time 1.6-9.7 years, 19% male) and 69 had been treated with atenolol (age 6.9-9.7 years, follow-up time 4.5-8.4 years, 19% male), were analyzed. The CPI and other neurocognitive outcomes did not differ between the propranolol and atenolol groups and were in line with general population test norms. Post hoc analyses revealed lower CPI scores for males, both compared to participating females (10.3 IQ points, medium effect size) and compared to matched test norms (12.4 IQ points, medium effect size).
CONCLUSIONS
Long-term neurocognitive functioning did not differ between children treated with propranolol and those treated with atenolol for IH. Overall, propranolol and atenolol appear to be safe treatments for IH regarding long-term neurocognitive functioning. The substantially lower CPI scores in males warrant further investigation.
TRIAL REGISTRATION
Netherlands Trial Register, NL7703 https://www.trialregister.nl/trial/7703 What is Known: • Infants with infantile hemangioma are effectively treated with propranolol or atenolol. • Parents and professionals are concerned about long-term neurocognitive effects.
WHAT IS NEW
• No long-term (≥ 6 years) differences in neurocognitive functioning were found between children treated with propranolol or atenolol. • Males treated with beta-blockers had substantially lower IQ scores than treated females and males from the general population, which is a matter of concern and should be considered when evaluating the risk/benefit ratio in less severe forms of infantile hemangioma.
Topics: Infant; Female; Humans; Male; Child; Propranolol; Atenolol; Cross-Sectional Studies; Adrenergic beta-Antagonists; Hemangioma; Treatment Outcome; Hemangioma, Capillary
PubMed: 36478294
DOI: 10.1007/s00431-022-04674-7 -
Molecules (Basel, Switzerland) Jun 2019A method based on gas chromatography-mass spectrometry (GC-MS) is described for the determination of bisoprolol and atenolol in human bone. After the addition of...
A method based on gas chromatography-mass spectrometry (GC-MS) is described for the determination of bisoprolol and atenolol in human bone. After the addition of lobivolol as internal standard, pulverized samples were incubated in acetonitrile for 1 h under ultrasounds. After adjusting the pH of the samples to 6, they were centrifuged, and the supernatants were subjected to solid phase extraction. Elution was achieved by using 3 mL of 2% ammonium hydroxide in 80:20 dichloromethane:isopropanol solution. Eluted samples were evaporated and derivatized. Chromatography was performed on a fused silica capillary column and analytes were determined in the selected-ion-monitoring (SIM) mode. The assay was validated in the range 0.1-0.3 ng/mg (depending on the drug) to 150 ng/mg, the mean absolute recoveries were 60% for bisoprolol and 106% for atenolol, the matrix effect was 69% for bisoprolol and 70% for atenolol and process efficiency was 41% for bisoprolol and 80% for atenolol. The intra- and inter-assay accuracy values were always better than 12%. The validated method was then applied to bone samples from two real forensic cases in which toxicological analysis in blood were positive for atenolol in the first case (0.65 µg/mL) and bisoprolol in the second case (0.06 µg/mL). Atenolol was found in bone samples from the corresponding case at the approximate concentration of 148 ng/mg and bisoprolol was found at 8 ng/mg.
Topics: Atenolol; Bisoprolol; Bone and Bones; Forensic Toxicology; Gas Chromatography-Mass Spectrometry; Humans; Reproducibility of Results; Solid Phase Extraction
PubMed: 31261852
DOI: 10.3390/molecules24132400 -
The Science of the Total Environment Mar 2022Atenolol is a widely prescribed beta-blocker that has been detected in wastewater at concentrations up to 300 μg/L. The parent compound and its transformation products...
Atenolol is a widely prescribed beta-blocker that has been detected in wastewater at concentrations up to 300 μg/L. The parent compound and its transformation products pose risks to aquatic organisms. Efficient atenolol degrading microorganism has yet to be identified, and its biodegradation pathway is unknown. In this study, Hydrogenophaga sp. YM1 isolated from activated sludge can degrade atenolol efficiently (286.1 ± 4.0 μg/g dry wt/h in actual wastewater), where atenolol acid, and four newly detected products (4-hydroxyphenylacetic acid, 3-(isopropylamino)-1,2-propanediol, 3-amino-1,2-propanediol and 4-(1-amino-2-hydroxy-3-propoxy) benzeneacetic acid) were the main intermediates. Key genes involved in atenolol degradation were proposed based on RNA-seq and validated by RT-qPCR. The ether bond cleavage of atenolol acid was the rate-limiting step likely catalyzed by the α-ketoglutarate dependent 2,4-dichlorophenoxyacetate dioxygenase. The further degradation of 4-hydroxyphenylacetic acid followed the homoprotocatechuate degradation pathway, enabling complete conversion to CO. Acetate addition (39-156 mg COD/L) under aerobic condition enhanced atenolol degradation by 29-37% and decreased the accumulation of atenolol acid, likely because acetate oxidation provided α-ketoglutarate and additional reducing power. Activated sludge core microorganisms have limited atenolol mineralization potentials. Enriching Hydrogenophaga-like populations and/or providing such as acetate can drive more complete conversion of atenolol in natural and engineered biosystems.
Topics: Atenolol; Biodegradation, Environmental; Comamonadaceae; Sewage; Wastewater
PubMed: 34890665
DOI: 10.1016/j.scitotenv.2021.152218 -
Lancet (London, England) Aug 2016Control of the heart rate (rate control) is central to atrial fibrillation management, even for patients who ultimately require control of the rhythm. We review heart... (Review)
Review
Control of the heart rate (rate control) is central to atrial fibrillation management, even for patients who ultimately require control of the rhythm. We review heart rate control in patients with atrial fibrillation, including the rationale for the intervention, patient selection, and the treatments available. The choice of rate control depends on the symptoms and clinical characteristics of the patient, but for all patients with atrial fibrillation, rate control is part of the management. Choice of drugs is patient-dependent. β blockers, alone or in combination with digoxin, or non-dihydropyridine calcium-channel blockers (not in heart failure) effectively lower the heart rate. Digoxin is least effective, but a reasonable choice for physically inactive patients aged 80 years or older, in whom other treatments are ineffective or are contraindicated, and as an additional drug to other rate-controlling drugs, especially in heart failure when instituted cautiously. Atrioventricular node ablation with pacemaker insertion for rate control should be used as an approach of last resort but is also an option early in the management of patients with atrial fibrillation treated with cardiac resynchronisation therapy. However, catheter ablation of atrial fibrillation should be considered before atrioventricular node ablation. Although rate control is a top priority and one of the first management issues for all patients with atrial fibrillation, many issues remain.
Topics: Adrenergic beta-Antagonists; Age Factors; Amiodarone; Anti-Arrhythmia Agents; Atenolol; Atrial Fibrillation; Atrioventricular Node; Bradycardia; Calcium Channel Blockers; Cardiac Resynchronization Therapy; Catheter Ablation; Digoxin; Drug Therapy, Combination; Heart Failure; Heart Rate; Humans; Pacemaker, Artificial; Patient-Centered Care; Practice Guidelines as Topic; Randomized Controlled Trials as Topic; Sotalol
PubMed: 27560277
DOI: 10.1016/S0140-6736(16)31258-2