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Environmental Science and Pollution... Mar 2014Atenolol is a β-blocker drug and an identified emerging pollutant. Advanced oxidation processes (AOPs) utilise the reaction of a highly oxidising species (hydroxyl...
Atenolol is a β-blocker drug and an identified emerging pollutant. Advanced oxidation processes (AOPs) utilise the reaction of a highly oxidising species (hydroxyl radicals, (•)OH) for the mineralisation of emerging pollutants since conventional treatment methodologies generally fail to degrade these compounds. In the present work, degradation of atenolol was carried out using ultrasound with frequencies ranging from 200 kHz to 1 MHz as a source of hydroxyl radical. The degradation was monitored by HPLC, total organic carbon (TOC) and chemical oxygen demand (COD) reduction and ion chromatography (IC). Nearly 90 % of degradation of atenolol was observed with ultrasound having 350 kHz. Both frequency and power of ultrasound affect the efficiency of degradation. Nearly 100 % degradation was obtained at a pH of 4. Presence of various additives such as sodium dodecyl sulphate, chloride, sulphate, nitrate, phosphate and bicarbonate was found to reduce the efficiency of degradation. Although nearly 100 % degradation of atenolol was observed under various experimental conditions, only about 62 % mineralisation (from TOC and COD measurements) was obtained. Nearly eight intermediate products were identified using high-resolution mass spectrometry (LC-Q-TOF). These products were understood as the results of hydroxyl radical addition to atenolol. The degradation studies were also carried out in river water which also showed a similar degradation profile. A mechanism of degradation and mineralisation is presented.
Topics: Atenolol; Biological Oxygen Demand Analysis; Fresh Water; Hydroxyl Radical; Models, Chemical; Nitrates; Oxidation-Reduction; Water Pollutants, Chemical
PubMed: 24306722
DOI: 10.1007/s11356-013-2301-x -
British Medical Journal May 1975The antihypertensive effect of atenolol, a new beta-1-receptor blocking agent, was studied in a double-blind trial in which 45 patients with essential hypertension were... (Clinical Trial)
Clinical Trial Comparative Study Randomized Controlled Trial
The antihypertensive effect of atenolol, a new beta-1-receptor blocking agent, was studied in a double-blind trial in which 45 patients with essential hypertension were randomly assigned to placebo or atenolol treatment. Atenolol caused a statistically significant and clinically relevant reduction of blood pressure. The optimum daily dose for moderately severe hypertension was considered to be 200 mg. Several irrelevant side effects were collected by the use of a check list, but there was no difference in the number of complaints during placebo and active treatment. Atenolol has a useful antihypertensive effect and, at least theoretically, has advantages over other beta-adrenergic blocking agents.
Topics: Adolescent; Adrenergic beta-Antagonists; Adult; Aged; Atenolol; Blood-Brain Barrier; Clinical Trials as Topic; Female; Humans; Hypertension; Male; Middle Aged; Placebos; Propanolamines
PubMed: 236810
DOI: 10.1136/bmj.2.5967.367 -
Glycoconjugate Journal Apr 2021Amongst a wide range of biological macromolecules, saccharides exhibit the potential to be specifically recognized by cell-surface receptors and hence can be utilized as...
Amongst a wide range of biological macromolecules, saccharides exhibit the potential to be specifically recognized by cell-surface receptors and hence can be utilized as ligands in targeted drug delivery. The current study aims to use saccharides viz. Galactose, Pectin and Chitosan to improve targeting of Atenolol by oxalyl chloride mediated grafting. Conjugates were engineered by grafting Atenolol, a cardiovascular agent with the modified saccharide units. The conjugates were characterized by FTIR, DSC and H NMR study. Drug release analysis and cellular uptake study was carried out using H9c2 cell lines which represent that concentration of drug in cells treated with all atenolol-saccharide conjugates is enhanced by almost two-folds in comparison with cells treated with atenolol solution. Thus cell line study confers the evidence of selective cardiac delivery. No significant cytotoxicity was observed in case of all synthesized conjugates in the Brine shrimp lethality bioassay. Possible binding of the developed conjugates with the GLUT-4 receptors was assessed by in silico analysis using homology model developed by Swiss Model server. Hence it was concluded that the application of these conjugates with saccharides in selective cardiovascular drug delivery can be a promising approach to increase bioavailability, minimize drug loss by degradation and prevent harmful side effects by increasing specific cell targeting.
Topics: Adrenergic beta-1 Receptor Antagonists; Animals; Artemia; Atenolol; Cell Line; Chitosan; Computer Simulation; Drug Carriers; Drug Evaluation, Preclinical; Galactose; Glucose Transporter Type 4; Lethal Dose 50; Magnetic Resonance Spectroscopy; Myocardium; Pectins; Rats; Spectroscopy, Fourier Transform Infrared
PubMed: 33687640
DOI: 10.1007/s10719-021-09983-x -
Annals of Internal Medicine Feb 1982
Comparative Study
Topics: Adrenergic beta-Antagonists; Atenolol; Humans; Hypertension; Kinetics; Propanolamines; Propranolol
PubMed: 6120670
DOI: 10.7326/0003-4819-96-2-244 -
Pediatric Cardiology 1996Propranolol, a first-generation nonselective beta-adrenoceptor blocking agent, is commonly used to treat pediatric arrhythmias. Atenolol, relatively long-acting,...
Propranolol, a first-generation nonselective beta-adrenoceptor blocking agent, is commonly used to treat pediatric arrhythmias. Atenolol, relatively long-acting, cardioselective beta-adrenoceptor blocking agent, has been successfully used in adults with supraventricular tachycardia (SVT). There is only one report on the use of atenolol in children with SVT; and our report is on the first long-term prospective study to evaluate the use of atenolol in children. A group of 22 children < 18 years of age with clinical SVT were enrolled in the study. The tachycardia was documented on electrocardiograms in each case and was confirmed by electrophysiologic studies in some. Once-a-day oral atenolol was started as a monotherapy. Of the 22 children with various types of SVT, 13 (59%) were well controlled on long-term oral atenolol therapy. The effective dose of atenolol ranged between 0.3 and 1.3 mg/kg/day (median effective dose 0.7 mg/kg/day). Five children had some adverse effects. However, none in the successful group of 13 patients required drug discontinuation because of such effects. Once-a-day oral atenolol as a monotherapy is effective and relatively safe for long-term management of SVT during childhood. It is an attractive alternative beta-adrenoceptor blocking agent for the management of pediatric arrhythmias.
Topics: Adolescent; Adrenergic beta-Antagonists; Atenolol; Child; Female; Humans; Male; Prospective Studies; Tachycardia, Supraventricular; Treatment Outcome
PubMed: 8662045
DOI: 10.1007/BF02524799 -
Biopharmaceutics & Drug Disposition 1983The pharmacokinetics of the cardioselective beta-adrenoreceptor blocking agent atenolol have been determined following intravenous and oral dosing to the dog. After...
The pharmacokinetics of the cardioselective beta-adrenoreceptor blocking agent atenolol have been determined following intravenous and oral dosing to the dog. After intravenous administration at 200 mg the blood levels of parent drug were found to decay tri-exponentially with a final elimination phase half-life of about 4.5 h. The volume of distribution for the central compartment was 40 per cent body weight and the whole body volume of distribution was 160 per cent body weight. The percentage urinary recovery of parent drug was 83 per cent. Following oral dosing at 400 mg (as a solution and as a clinical trial tablet) the percentage urinary recovery was 65 per cent and the half-life extended slightly to between 5 and 6 h. The peak blood levels were however very similar for the two formulations (17 and 15 micrograms/ml for the solution and tablet respectively) and occurred at the same time (1-2 h after dosing). The total ares under the blood concentration time curves were similar and the values (100 and 104 micrograms/ml-1 h respectively) agreed well with that anticipated on the basis of the intravenous data. It was concluded that the two formulations were bioequivalent and that following oral dosing atenolol was almost completely absorbed with little metabolism or biliary excretion. Following chronic oral dosing at 50, 100, and 200 mg/kg/day the systemic blood levels were found to increase with dose at all time points throughout the study. There was no sex or dose dependency of the half-life and its value on chronic dosing was very similar to that on acute dosing. The dose dependency of the area under the blood concentration time curves was reflected in the plateau blood levels and there was very good agreement between the experimental values and the theoretical relationship based on the acute pharmacokinetic data. In accordance with the half-life there was no accumulation at any of the dose levels studied. Thus it can be concluded that atenolol obeys linear pharmacokinetics over the dose range studied.
Topics: Animals; Atenolol; Biological Availability; Capsules; Dogs; Half-Life; Injections, Intravenous; Kinetics; Male; Tablets
PubMed: 6626700
DOI: 10.1002/bdd.2510040306 -
European Journal of Clinical... 1984After screening a local population in the northern part of The Netherlands for hypertension, 119 patients with a diastolic pressure (DP) between 95 and 120 mmHg were... (Clinical Trial)
Clinical Trial Comparative Study Randomized Controlled Trial
After screening a local population in the northern part of The Netherlands for hypertension, 119 patients with a diastolic pressure (DP) between 95 and 120 mmHg were randomised and treated either with 50 mg hydrochlorothiazide (n = 59) or 100 mg atenolol (n = 60). After 1 month of treatment 6 patients in the hydrochlorothiazide group and 24 patients in the atenolol group had reached a DP less than or equal to 90 mmHg (p less than 0.001). 43 of the 50 non-responders to hydrochlorothiazide were switched to atenolol and 30 of the 35 non-responders to atenolol were changed to hydrochlorothiazide. One month after the switch 19 patients in the atenolol group and 2 patients in the hydrochlorothiazide group had reached a DP less than or equal to 90 mmHg (p less than 0.001). After 6 months of treatment 32 of the 43 atenolol responders and 7 of the 8 hydrochlorothiazide responders were still receiving the same medication, as their DP was still less than or equal to 90 mmHg. Non-responders to either medication were given the combination (n = 46). 21 patients now became normotensive as did a further 10 after increasing the dose of atenolol to 200 mg. Thus, in all 70 patients had a blood pressure less than or equal to 90 mmHg after treatment for 4 months. Both drugs induced a significant reduction in the total of number of complaints after 1 month of treatment. They did not differ from each other. The reduction was seen both in responders and non-responders and persisted during treatment for 6 months. It is concluded that in terms of short-term efficacy the cardioselective, hydrophilic beta adrenoceptor-blocking drug atenolol is preferable to hydrochlorothiazide in the treatment of uncomplicated hypertension.
Topics: Adult; Atenolol; Blood Pressure; Clinical Trials as Topic; Female; Half-Life; Humans; Hydrochlorothiazide; Hypertension; Male; Middle Aged
PubMed: 6373303
DOI: 10.1007/BF00630280 -
Journal of Cellular and Molecular... Apr 2009Combinations therapy is often used in hypertensive patients whether combination therapy is necessary for preventing end-organ damage is not known. The objective of this...
Combinations therapy is often used in hypertensive patients whether combination therapy is necessary for preventing end-organ damage is not known. The objective of this study was to determine in four different hypertensive animal models the necessity of adding the calcium channel blocker amlodipine to therapy with the ss-blocker atenolol to modulate end-organ damage. Spontaneously hypertensive rats, DOCA-salt hypertensive rats, two-kidney, one-clip renovascular hypertensive rats and Lyon genetically hypertensive rats were used to study this objective. These animal models have different sensitivities to atenolol and amlodipine. The dosages of therapy employed were 10 mg/kg atenolol alone, 1 mg/kg amlodipine, 10 mg atenolol + 1 mg/kg amlodipine and 5 mg/kg atenolol+0.5 mg/kg amlodipine. BP was continuously recorded in all animals. After determination of baroreflex sensitivity, rats were sacrificed for end-organ damage evaluation. The combination of amlodipine and atenolol had a synergistic inhibitory effect on blood pressure and blood pressure variability, and end-organ damage as compared with monotherapy with atenolol or amlodipine in all animal models. Baroreflex sensitivity also improved with the combination therapy more than with monotherapy. In conclusion, atenolol and amlodipine combination exerts a superior effect on blood pressure, blood pressure variability, baroreflex sensitivity and end-organ damage. The superior effect of the combination was observed in all four models of hypertension.
Topics: Amlodipine; Animals; Atenolol; Blood Pressure; Drug Therapy, Combination; Hemodynamics; Hypertension; Male; Organ Specificity; Rats; Rats, Sprague-Dawley; Regression Analysis; Time Factors
PubMed: 19220584
DOI: 10.1111/j.1582-4934.2008.00365.x -
British Journal of Clinical Pharmacology Sep 1990
Clinical Trial Randomized Controlled Trial
Topics: Adult; Atenolol; Drug Interactions; Female; Humans; Male; Nicardipine
PubMed: 2223431
DOI: 10.1111/j.1365-2125.1990.tb03806.x -
Journal of Clinical Pharmacology Mar 1995The negative inotropic and chronotropic effects of beta-blocker therapy have been reported to reduce morbidity and mortality in patients with Marfan syndrome; however,... (Comparative Study)
Comparative Study
The negative inotropic and chronotropic effects of beta-blocker therapy have been reported to reduce morbidity and mortality in patients with Marfan syndrome; however, little is known about the pharmacokinetics of atenolol after oral administration of multiple doses to patients with the Marfan syndrome. We studied the pharmacokinetics of atenolol in 13 such patients aged 18.7 +/- 2.9 years who were receiving 1.78 +/- 0.58 mg/kg/day (70.1 +/- 20.3 mg/m2/day) of atenolol for 6 weeks or longer. Mean +/- SD percentage change in baseline heart rate after the administration of atenolol was -18.03 +/- 16.59% and mean +/- SD percentage change in exercise heart rate after atenolol was -33.22 +/- 14.75% (P < .01). Six to 8 atenolol serum concentrations were collected in each patient during a 12-hour dosing interval and were determined by high-performance liquid chromatography with ultraviolet detection. Serum atenolol concentrations at 0 (123 +/- 70 micrograms/L) and 12 (116 +/- 66 micrograms/L) hours were within 20% of each other and were thus assumed to be at steady-state. A one-compartment, steady-state pharmacokinetic model with first-order absorption and elimination was fitted to the concentration-time data for each patient using nonlinear regression. Maximal concentration was 343 +/- 120 micrograms/L, and the mean half-life was 4.72 hours.(ABSTRACT TRUNCATED AT 250 WORDS)
Topics: Absorption; Administration, Oral; Adolescent; Adult; Atenolol; Drug Administration Schedule; Exercise Test; Half-Life; Heart Rate; Humans; Marfan Syndrome; Metabolic Clearance Rate
PubMed: 7608315
DOI: 10.1002/j.1552-4604.1995.tb04057.x