The Experts below are selected from a list of 3078 Experts worldwide ranked by ideXlab platform
P. Jaillon - One of the best experts on this subject based on the ideXlab platform.
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A comparative pharmacokinetic and pharmacodynamic study of conventional and sustained-release preparations of Acebutolol in healthy volunteers.
Fundamental & clinical pharmacology, 1991Co-Authors: O. Fleurot, B. Lecocq, V. Lecocq, A. Le Liboux, G. Montay, A. Frydman, P. JaillonAbstract:Pharmacokinetics and the degree of beta-blockade of sustained release (SR) Acebutolol (500 mg/day) and conventional Acebutolol (200 mg tid) were examined after the first oral dose and after 10 days of treatment in ten healthy volunteers. After the first dose, Acebutolol Cmax did not significantly differ between the two formulations; however, on day 10 Acebutolol Cmax was significantly higher after SR formulation. Cmax of diacetolol, the major metabolite, did not differ between SR and conventional Acebutolol neither on day 1 nor on day 10. The dose-corrected relative bio-availability of Acebutolol was not different from 100% on day 1 and day 10; however the dose-corrected diacetolol AUC, SR/conventional ratio, was significantly lower than 100% on days 1 and 10. Both Acebutolol preparations exerted a significant reduction in exercise tachycardia over 24 h on day 1 and day 10; however, conventional Acebutolol exhibited a greater reduction 24 h after the first dose. Exercise-induced increase in systolic blood pressure was similarly inhibited by both treatments except for 24 h after the first dose when systolic blood pressure was significantly higher with SR than with conventional Acebutolol. The percent reduction in heart rate during exercise was linearly correlated with log Acebutolol plasma concentrations for each treatment regimen. These results suggest that beta-blockade exerted by SR Acebutolol in healthy volunteers is equivalent to that of conventional Acebutolol.
Alain Leizorovicz - One of the best experts on this subject based on the ideXlab platform.
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persistent reduction of mortality for five years after one year of Acebutolol treatment initiated during acute myocardial infarction
American Journal of Cardiology, 1997Co-Authors: Michel Cucherat, Jeanpierre Boissel, Alain LeizoroviczAbstract:Abstract The APSI trial was a randomized placebo-controlled trial designed to assess the efficacy of 1 year of treatment by Acebutolol in high-risk patients who had survived an acute myocardial infarction. At 1 year there was a statistically significant 48% relative reduction in total mortality (p = 0.019) in favor of Acebutolol. In 1995 a long-term mortality survey was undertaken through an administrative inquiry and contacts with investigators. The vital status of 586 of the 607 (96.5%) patients enrolled was known at the cutoff date and all these patients were followed up for at least 5 years. During follow-up (in-trial and post-trial period), 74 deaths (24.8%) occurred in the Acebutolol group and 96 (31.1%) in the placebo group (p = 0.10). No difference between the 2 groups was observed for the number of deaths that occurred after the end of the trial: 55 deaths (19.6%) among the 281 survivors in the Acebutolol group and 59 deaths (21.7%) (p = 0.70) among the 272 survivors in the placebo group. The annual hazard rate (annual death rate), calculated year by year using the actuarial method, was significantly different (p The APSI trial was a randomized placebo-controlled trial designed to assess the efficacy of 1-year treatment by Acebutolol in high-risk patients who had survived an acute myocardial infarction. The present long-term mortality survey shows that the initial benefit conferred by Acebutolol during the first year after myocardial infarction treatment is maintained for 5 years.
Jonathan F. Dreyer - One of the best experts on this subject based on the ideXlab platform.
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Acebutolol-induced ventricular tachycardia reversed with sodium bicarbonate.
Clinical Toxicology, 1999Co-Authors: Keith D. Donovan, Rocco V. Gerace, Jonathan F. DreyerAbstract:Background: Acebutolol is a unique beta blocker that possesses cardioselectivity, partial agonist activity, and membrane stabilizing activity. Sodium bicarbonate is used to reverse the cardiotoxic effects of other drugs with membrane stabilizing activity. There have been no reported cases of Acebutolol-induced ventricular dysrhythmias treated successfully with bolus sodium bicarbonate. Case Presentation: A 48-year-old man ingested approximately 6.4 g of Acebutolol with ethanol (blood ethanol 61 mmol/L). There were no other coingestants identified. One hour after presentation, the patient had a cardiac arrest with the monitor showing ventricular tachycardia. Sodium bicarbonate 50 mEq intravenous push converted the patient to sinus rhythm and the blood pressure improved to 129/90 mm Hg. Conclusion: This case demonstrates a temporal relationship between bolus sodium bicarbonate administration and the termination of Acebutolol-induced ventricular tachycardia.
Kheng Soo Tay - One of the best experts on this subject based on the ideXlab platform.
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Aqueous chlorination of Acebutolol: kinetics, transformation by-products, and mechanism.
Environmental science and pollution research international, 2015Co-Authors: Wan Nor Adira Wan Khalit, Kheng Soo TayAbstract: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 Acebutolol and free available chlorine was increased from 1.68 to 11.2 M(-1) min(-1). By comparing with the reported k app values, the reactivity of Acebutolol toward free available chlorine was found to be higher than atenolol and metoprolol but lower than nadolol and propranolol. Characterization of the transformation by-products formed during the chlorination of Acebutolol was carried out using liquid chromatography-quadrupole time-of-flight high-resolution mass spectrometry. Seven major transformation by-products were identified. These transformation by-products were mainly formed through dealkylation, hydroxylation, chlorination, and oxidation reactions.
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Ozonation of Acebutolol in aqueous solution: Ozonation by-products and degradation pathway
Separation and Purification Technology, 2014Co-Authors: Kheng Soo Tay, Norfazrina MadehiAbstract:Abstract Ozonation is one of the common methods for pollutant removal and disinfection in water treatment. The reaction between the ozone and organic pollutants involves complex oxidation pathway which may lead to the formation of various ozonation by-products. In some cases, toxic ozonation by-products may be produced. In this study, the ozonation by-products of Acebutolol, one of the common β-blockers, were identified. The mechanisms for the transformation of Acebutolol during ozonation were elaborated. In this study, ozonation was carried out at pH 2 (with the presence of radical scavenger), 7 and 12, in order to study the role of the ozone (O 3 ) and hydroxyl radical ( OH) in the transformation of Acebutolol. Structure elucidation of the ozonation by-products was carried out using HPLC coupled with quadrupole time-of-flight high resolution mass spectrometry. Sixteen ozonation by-products were identified, of which fifteen have never been reported elsewhere. Based on the detected ozonation by-products, Acebutolol can be degraded by both O 3 and OH. When the O 3 itself becomes a reactive species, the transformation of the Acebutolol proceeded via the reaction between the O 3 and the aromatic ring of the Acebutolol to form the aromatic ring hydroxylated and aromatic ring opening by-products. Without the radical scavenger, ozonation at pH 7 and 12 showed that the transformation of the Acebutolol proceeded via the involvement of the OH and different aliphatic chain degraded and hydroxylated by-products were detected.
Pertti J Neuvonen - One of the best experts on this subject based on the ideXlab platform.
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effects of grapefruit juice on the pharmacokinetics of Acebutolol
British Journal of Clinical Pharmacology, 2005Co-Authors: Jari J Lilja, Kari Raaska, Pertti J NeuvonenAbstract:Aims We aimed to investigate effects of grapefruit juice on Acebutolol pharmacokinetics. Methods In a randomized cross-over study, 10 healthy subjects ingested 200 mL grapefruit juice or water three times daily for 3 days and twice on day 4. On day 3, each subject ingested 400 mg Acebutolol with grapefruit juice or water. The concentrations of Acebutolol and its metabolite diacetolol were measured in plasma and urine up to 33 h. Results Grapefruit juice decreased the peak plasma concentration (Cmax) of Acebutolol by 19% from 872 ± 207 ng mL−1 to 706 ± 140 ng mL−1 (95% CI on the difference −306, −26.4; P < 0.05), and the area under the concentration time curve (AUC0−33 h) by 7%, from 4498 ± 939 ng mL−1 h to 4182 ± 915 ng mL−1 h (95% CI −609, −23.0; P < 0.05). The half-life (t1/2) of Acebutolol prolonged from 4.0 to 5.1 h (P < 0.05). The time to peak concentration and the amount of Acebutolol excreted into urine (Ae) were unchanged. The Cmax, AUC0−33 h, and Ae of diacetolol were decreased by 24% (P < 0.05), 18% (P < 0.05), and 20% (P < 0.01), respectively, by grapefruit juice. Conclusion Grapefruit juice caused a small decrease in the plasma concentrations of Acebutolol and diacetolol by interfering with gastrointestinal absorption. The interaction between the grapefruit juice and Acebutolol is unlikely to be of clinical significance in most of the patients.
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Effects of grapefruit juice on the pharmacokinetics of Acebutolol
British journal of clinical pharmacology, 2005Co-Authors: Jari J Lilja, Kari Raaska, Pertti J NeuvonenAbstract:Aims We aimed to investigate effects of grapefruit juice on Acebutolol pharmacokinetics. Methods In a randomized cross-over study, 10 healthy subjects ingested 200 mL grapefruit juice or water three times daily for 3 days and twice on day 4. On day 3, each subject ingested 400 mg Acebutolol with grapefruit juice or water. The concentrations of Acebutolol and its metabolite diacetolol were measured in plasma and urine up to 33 h. Results Grapefruit juice decreased the peak plasma concentration (Cmax) of Acebutolol by 19% from 872 ± 207 ng mL−1 to 706 ± 140 ng mL−1 (95% CI on the difference −306, −26.4; P
