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P. Jaillon – One of the best experts on this subject based on the ideXlab platform.
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.
persistent reduction of mortality for five years after one year of Acebutolol treatment initiated during acute myocardial infarctionAmerican 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.
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.