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The American Journal of Cardiology Jan 1979The effect of intravenous acebutolol versus saline solution on frequent premature ventricular complexes was evaluated in a double-blind, randomized study in 20 patients,... (Clinical Trial)
Clinical Trial Randomized Controlled Trial
The effect of intravenous acebutolol versus saline solution on frequent premature ventricular complexes was evaluated in a double-blind, randomized study in 20 patients, including 3 with chronic obstructive pulmonary disease. Frequent premature ventricular complexes were abolished or reduced by 75% or more in none of 12 patients given saline solution but in 18 of 20 patients (90%) given acebutolol (P less than 0.001). This therapeutic effect of acebutolol persisted for at least 2.5 hours in 17 of 20 patients (85%), for at least 3.5 hours in 14 (70%) and for at least 4 hours in 8 (40%). Acebutolol was well tolerated by the three patients with chronic obstructive pulmonary disease. These data indicate that intravenous acebutolol is useful in the treatment of premature ventricular complexes.
Topics: Acebutolol; Adult; Aged; Arrhythmias, Cardiac; Double-Blind Method; Drug Evaluation; Humans; Injections, Intravenous; Male; Middle Aged; Placebos
PubMed: 758758
DOI: 10.1016/0002-9149(79)90052-3 -
American Heart Journal Feb 1985A multicenter, double-blind study compared oral acebutolol (n = 186) with propranolol (n = 190) in the treatment of mild to moderately severe essential hypertension... (Clinical Trial)
Clinical Trial Comparative Study Randomized Controlled Trial
A multicenter, double-blind study compared oral acebutolol (n = 186) with propranolol (n = 190) in the treatment of mild to moderately severe essential hypertension (diastolic greater than or equal to 95 to 129 mm Hg). Both beta blockers produced significant and comparable reductions in diastolic, systolic, and mean arterial blood pressures of 16%, 12%, and 14% on acebutolol and 15%, 12%, and 14% on propranolol (all p less than 0.01). At equipotent, antihypertensive doses, acebutolol induced significantly less reduction in resting heart rate than propranolol (13% on acebutolol, 17% on propranolol, p = 0.02). The mean effective doses of acebutolol and propranolol were 738 mg and 231 mg, respectively. Significantly fewer acebutolol patients experienced central nervous system side effects (acebutolol, n = 50; propranolol, n = 75; p = 0.01) or withdrew from the study prematurely due to side effects (acebutolol, n = 11; propranolol, n = 29; p less than 0.01). No clinically significant trends in abnormalities of laboratory parameters were seen, and there were no statistically significant differences in the development of positive antinuclear antibody titers between the two treatment groups. It is concluded that acebutolol is as effective as propranolol in the treatment of hypertension, and acebutolol was better tolerated on the basis of heart rate and central nervous system side effects.
Topics: Acebutolol; Adult; Aged; Antibodies, Antinuclear; Blood Pressure; Body Weight; Clinical Trials as Topic; Double-Blind Method; Female; Heart Rate; Humans; Hypertension; Male; Middle Aged; Propranolol
PubMed: 3880995
DOI: 10.1016/0002-8703(85)90600-3 -
Chirality Jun 2015A new chemoenzymatic route is reported to synthesize acebutolol, a selective β1 adrenergic receptor blocking agent in enantiopure (R and S) forms. The enzymatic kinetic...
A new chemoenzymatic route is reported to synthesize acebutolol, a selective β1 adrenergic receptor blocking agent in enantiopure (R and S) forms. The enzymatic kinetic resolution strategy was used to synthesize enantiopure intermediates (R)- and (S)-N-(3-acetyl-4-(3-chloro-2-hydroxypropoxy)phenyl)butyramide from the corresponding racemic alcohols. The results showed that out of eleven commercially available lipase preparations, two enzyme preparations (Lipase A, Candida antarctica, CLEA [CAL CLEA] and Candida rugosa lipase, 62316 [CRL 62316]) act in enantioselective manner. Under optimized conditions the enantiomeric excess of both (R)- and (S)-N-(3-acetyl-4-(3-chloro-2-hydroxypropoxy)phenyl)butyramide were 99.9 and 96.8%, respectively. N-alkylation of both the (R) and (S) intermediates with isopropylamine gave enantiomerically pure (R and S)- acebutolol with a yield 68 and 72%, respectively. This study suggests a high yielding, easy and environmentally green approach to synthesize enantiopure acebutolol.
Topics: Acebutolol; Adrenergic beta-1 Receptor Antagonists; Biocatalysis; Models, Biological; Molecular Structure; Stereoisomerism; Substrate Specificity
PubMed: 25977108
DOI: 10.1002/chir.22444 -
Journal of Chromatography. A Jul 2005Acebutolol [N-{3-acetyl-4-[(2-hydroxy-3-(isopropylamino)propoxy]phenyl} butanamide] is a cardioselective beta-blocker with a potent anti-hypertensive and antiarrhythmic...
Acebutolol [N-{3-acetyl-4-[(2-hydroxy-3-(isopropylamino)propoxy]phenyl} butanamide] is a cardioselective beta-blocker with a potent anti-hypertensive and antiarrhythmic effect. The optimised operational system of electrolytes for the newly developed ITP separation of acebutolol consisted of 10mM potassium acetate +10mM acetic acid (pH 4.65) as the leading electrolyte and 10mM beta-alanine with pH approximately 4 (adjusted with acetic acid) as the terminating electrolyte. The driving and detection currents were 75 and 20 microA, respectively and the analysis took approximately 13 min. Under these conditions the effective mobility of acebutolol was determined as 20.7 x 10(-9) m2 V(-1) s(-1). The calibration dependence was rectilinear in the range 0.14-1.4 mg ml(-1) of acebutolol base (r = 0.9995); relative standard deviation (RSD) values were 1.1% and 1.2% (n = 6) when determining 0.42 and 0.98 mg ml(-1) of acebutolol in a pure standard solution. The method, with the limit of detection (LOD) of 0.04 mg ml(-1) and limit of quantification (LOQ) of 0.12 mg ml(-1), was applied to the assay of acebutolol in Sectral tablets, Acecor tablets, Apo-acebutol tablets (nominal content 400 mg of acebutolol per tablet) and Acebirex tablets (nominal content 200 mg of acebutolol per tablet) with RSD = 0.7-1.7% (n = 6). No interference from any excipients present in the tablets was observed. The recoveries ranged from 98.8% to 102.4% as found by the standard addition technique.
Topics: Acebutolol; Adrenergic beta-Antagonists; Electric Conductivity; Electrolytes; Electrophoresis, Capillary; Hydrogen-Ion Concentration; Pharmaceutical Preparations; Reproducibility of Results; Sensitivity and Specificity
PubMed: 16013601
DOI: 10.1016/j.chroma.2005.04.034 -
European Annals of Otorhinolaryngology,... Nov 2011Infantile haemangioma (IH) is the most common tumour during early childhood. Although these benign lesions resolve spontaneously, up until recently laryngotracheal sites... (Review)
Review
Infantile haemangioma (IH) is the most common tumour during early childhood. Although these benign lesions resolve spontaneously, up until recently laryngotracheal sites of IH required invasive management. The dramatic efficacy of β-blockers on IH has radically changed the prognosis. Surgery is now no longer indicated as first-line therapy, but should only be performed for difficult, refractory cases, or in the presence of absolute contraindications to β-blockers. Long-term steroid therapy is also no longer indicated. Propranolol can be used as first-line, single-agent therapy.
Topics: Acebutolol; Adrenergic beta-Antagonists; Dose-Response Relationship, Drug; Hemangioma; Humans; Infant; Laryngeal Neoplasms; Laryngoscopy; Propranolol; Tracheal Neoplasms
PubMed: 21498145
DOI: 10.1016/j.anorl.2010.11.009 -
The American Journal of Cardiology Sep 1990A randomized, placebo-controlled trial was carried out to determine the effectiveness of acebutolol in preventing late death in high-risk patients surviving an acute... (Clinical Trial)
Clinical Trial Randomized Controlled Trial
A randomized, placebo-controlled trial was carried out to determine the effectiveness of acebutolol in preventing late death in high-risk patients surviving an acute myocardial infarction (MI). The average 1-year mortality rate in placebo groups of 9 trials of beta blockers in post-MI patients was 7.2% compared with 17% in a nonselected cohort of patients who had survived at least 7 days after an MI. The mandate for this trial was based on the fact that high-risk patients whose mortality rate exceeds 20% have not been enrolled in significant numbers in previous trials. It remains to be proved whether beta-blocking therapy in this patient population is beneficial. Selection of high-risk patients for inclusion in the trial was based on an algorithm set up from the Essai de Prevention Secondaire de l'Infarctus du Myocarde Registry. At the time of the second interim analysis, the mortality rate in the placebo group was 12%, lower than expected (greater than or equal to 20%). The trial was stopped; at that time, 309 patients had been allocated to placebo and 298 patients to acebutolol therapy. After 318 days, there were 17 deaths in the acebutolol-treated group and 34 in the placebo group, a reduction in total mortality of 48% (p = 0.019). There were 30 vascular deaths in the placebo group and 12 in the acebutolol group. Thus, cardiovascular mortality with acebutolol was reduced by 58% (p = 0.006). The incidence of all cardiovascular-related deaths was lower in the acebutolol-treated group. The total reduction in mortality did not appear to be correlated with secondary risk factors.(ABSTRACT TRUNCATED AT 250 WORDS)
Topics: Acebutolol; Algorithms; Contraindications; Double-Blind Method; Female; Humans; Male; Middle Aged; Myocardial Infarction; Prognosis; Risk Factors; Sympathetic Nervous System; Time Factors
PubMed: 2220646
DOI: 10.1016/0002-9149(90)90759-t -
European Journal of Clinical... 1986The concentrations of acebutolol and of its main active metabolite diacetolol in milk and plasma were studied in 7 hypertensive mothers treated with acebutolol, a...
The concentrations of acebutolol and of its main active metabolite diacetolol in milk and plasma were studied in 7 hypertensive mothers treated with acebutolol, a cardioselective beta-adrenoceptor blocking agent. Clinical monitoring on their newborn babies was also done, as well as measurement of plasma level of the drug in them. The ratio between milk and plasma concentrations ranged from 1.9 to 9.2 for acebutolol and from 2.3 to 24.7 for diacetolol, and in any given milk sample, the diacetolol concentration was always higher than that of acebutolol. In a newborn infant, plasma concentrations of the two transplacentally acquired substances was raised when breast feeding started and remained high. Clinical signs of pharmacological beta-blockade were observed. Evaluation of the iatrogenic risk shows that pharmacologically active amounts of acebutolol might be received by a neonate if the daily maternal dosage exceeds 400 mg/day and/or renal function in the mother is impaired.
Topics: Acebutolol; Breast Feeding; Female; Humans; Hypertension; Infant, Newborn; Milk, Human; Postpartum Period; Pregnancy; Prospective Studies
PubMed: 3770068
DOI: 10.1007/BF00608227 -
American Heart Journal May 1985The safety and efficacy of oral acebutolol therapy for the suppression of premature ventricular contractions (PVCs) were assessed in two clinical trials pooled for... (Comparative Study)
Comparative Study
The safety and efficacy of oral acebutolol therapy for the suppression of premature ventricular contractions (PVCs) were assessed in two clinical trials pooled for analysis. Thirty-two patients suffering from organic heart disease, who had experienced an average of greater than or equal to 10 PVCs/h (range 14 to 996 three times a day) on Holter monitoring during a 24-hour baseline study period, were given acebutolol (100 mg three times a day to 400 mg four times a day) over 4 weeks. Three patients were withdrawn from the study for administrative reasons, and four patients were excluded from the efficacy analysis. Of the 25 remaining patients (24 men, 1 woman; mean age 56 years, range 37 to 69), 18 (72%) experienced some reduction in PVCs from the second through the fourth week of therapy. Eleven patients (44%) experienced clinically significant reductions (greater than or equal to 75%) in PVCs. The onset of the antiarrhythmic effect of acebutolol was within 7 days of administration. Transient mild to moderate side effects were noted in eight patients. Significant correlations (p less than 0.001) were observed between the mean daily dose of acebutolol and (1) mean blood levels, (2) reduction in PVCs, and (3) reduction in resting heart rate. The average daily dose of acebutolol ranged from 304 to 1060 mg. In nine patients receiving acebutolol in a 12-month open-label extension, both efficacy and safety were maintained. This study confirms that oral acebutolol therapy in both safe and efficacious for suppressing PVCs in patients with organic heart disease.
Topics: Acebutolol; Adult; Aged; Arrhythmias, Cardiac; Female; Humans; Male; Middle Aged; Time Factors
PubMed: 3993536
DOI: 10.1016/0002-8703(85)90710-0 -
The New Zealand Medical Journal Apr 1979Eleven patients with hypertension and varying degrees of stable renal functional impairment were treated with the beta adrenoreceptor blocking drug, acebutolol...
Eleven patients with hypertension and varying degrees of stable renal functional impairment were treated with the beta adrenoreceptor blocking drug, acebutolol (Sectral). Parameters of renal, cardiovascular and respiratory function were measured immediately prior to treatment and again after four and 12 weeks. In five patients the blood pressure was well controlled throughout the 12-week period on 400mg of acebutolol each morning, in three the blood pressure was satisfactory after four weeks treatment with 400mg each morning but control had been lost by 12 weeks, while in the remaining three patients 800mg each morning was ineffective. There was no significant change in the mean glomerular filtration rate of the 11 patients but in two of these patients with severe, but stable, chronic renal failure the introduction of acebutolol was associated with a decline in renal function and the onset of uraemic symptoms. One of these patients showed an improvement when the acebutolol was discontinued but the other required regular dialysis treatment. Beta adrenoreceptor blockers should be used cautiously in severe renal failure.
Topics: Acebutolol; Adult; Aged; Female; Glomerular Filtration Rate; Humans; Hypertension, Renal; Male; Middle Aged
PubMed: 286923
DOI: No ID Found -
Clinical Pharmacology and Therapeutics Feb 1981We assessed the effects of acebutolol, a cardioselective beta blocker, on global and regional left ventricular function in 26 patients with chronic angina pectoris. All... (Clinical Trial)
Clinical Trial
We assessed the effects of acebutolol, a cardioselective beta blocker, on global and regional left ventricular function in 26 patients with chronic angina pectoris. All patients underwent rest and maximal supine bicycle exercise radionuclide angiography while on placebo and oral acebutolol (400 mg three times a day). Resting ejection fraction on placebo was 51 +/- 3% and on acebutolol was 54 +/- 3% (p less than 0.05). No resting ejection fraction decreased greater than or equal to 7%. Only one patient (resting ejection fraction 28% on placebo and 21% on acebutolol) developed signs of fluid retention. Exercise nuclear studies on placebo revealed responses consistent with coronary artery disease (abnormal ejection fraction response to exercise and regional wall motion abnormalities) in 24 of 26 patients. Peak exercise ejection fraction was of the same order on placebo and acebutolol (51 +/- 3% and 54 +/- 3%, p = NS). In four patients the ejection fraction response to exercise became normal and in five patients all regional wall motion abnormalities became normal on acebutolol. Cardioselective beta blockade with acebutolol in effective antianginal doses is safe and may improve resting and exercise ventricular function.
Topics: Acebutolol; Angina Pectoris; Blood Pressure; Coronary Disease; Coronary Vessels; Exercise Test; Heart; Heart Rate; Humans; Male; Radionuclide Imaging; Stroke Volume
PubMed: 7460480
DOI: 10.1038/clpt.1981.24