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International Journal of Cardiology Feb 1986We studied the effect of intravenous (1 mg/kg) and oral (400 mg) acebutolol on atrioventricular conduction in 22 patients with idiopathic bundle branch block and 1 to 1...
We studied the effect of intravenous (1 mg/kg) and oral (400 mg) acebutolol on atrioventricular conduction in 22 patients with idiopathic bundle branch block and 1 to 1 atrioventricular conduction. Seven patients had previously symptomatic complete heart block (Group 1) and 15 were asymptomatic with bundle branch block only (Group 2). Following intravenous acebutolol heart rate decreased 82 +/- 16 to 63 +/- 16/min (P less than 0.01), A-H interval lengthened 98 +/- 22 to 121 +/- 30 msec (P less than 0.005) and H-V time was prolonged 60 +/- 13 to 70 +/- 17 msec (P less than 0.02) in those with previous heart block. The corresponding changes in the patients with no previous block were 74 +/- 14 to 61 +/- 8/min (P less than 0.01), 90 +/- 17 to 109 +/- 22 msec (P less than 0.05) and 48 +/- 15 to 56 +/- 14 msec (P less than 0.01). There was no difference between the basal or induced changes between these two groups. After intravenous acebutolol infusion 2 of 6 patients with previous spontaneous heart block and none of those without previous heart block developed atrioventricular block distal to His. The induced block was temporary (less than 10 min) and corresponded to the time of peak plasma acebutolol levels. Temporary atrioventricular block followed oral acebutolol administration in 4/7 patients with previous spontaneous heart block and 0/14 in those without block. In patients with bundle branch block intravenous acebutolol prolonged H-V conduction times in 19/20 patients and intravenous and oral acebutolol induced A-V block in 4/7 patients with previous spontaneous block.(ABSTRACT TRUNCATED AT 250 WORDS)
Topics: Acebutolol; Administration, Oral; Adult; Aged; Blood Pressure; Bundle of His; Bundle-Branch Block; Female; Heart Rate; Humans; Infusions, Parenteral; Male; Middle Aged; Purkinje Fibers
PubMed: 3943932
DOI: 10.1016/0167-5273(86)90219-6 -
Journal of Clinical Pharmacology Oct 1993The selectivity of acebutolol, atenolol, and metoprolol in healthy volunteers was estimated by determining the extent to which the drugs occupied beta 1-receptors of... (Clinical Trial)
Clinical Trial Comparative Study Randomized Controlled Trial
The selectivity of acebutolol, atenolol, and metoprolol in healthy volunteers was estimated by determining the extent to which the drugs occupied beta 1-receptors of rabbit lung and beta 2-receptors of rat reticulocytes in the circulating plasma after drug intake. This ex vivo method had the advantage of including all drug components contributing to the drug-receptor equilibrium in vivo and of excluding the factors regulating organ sensitivity to catecholamine stimulation. The oral doses of 400 mg acebutolol, 100 mg atenolol, and 100 mg metoprolol were administered to six healthy male volunteers using a double-blind, randomized, and cross-over study design. The three drugs occupied beta 1-receptors to a similar extent at 2 hours after drug intake. The receptor fraction occupied by metoprolol at 3 to 8 hours after drug intake was usually smaller, however (analysis of variance for repeated measures, P < .05) than that of the other drugs. Acebutolol occupied significantly larger fractions of beta 2-receptors (analysis of variance for repeated measures, P < .05) than did atenolol and metoprolol. Therefore, at an identical beta 1-receptor occupancy, the beta 2-receptor occupancy of acebutolol was larger than that of the other agents. Apparently, active metabolites decreased markedly the selectivity of acebutolol, but not that of metoprolol. The receptor occupancy of the agents was well in agreement with the literature concerning the selectivity, intensity, and time-course of drug actions after identical doses.(ABSTRACT TRUNCATED AT 250 WORDS)
Topics: Acebutolol; Administration, Oral; Adult; Animals; Atenolol; Double-Blind Method; Humans; Male; Metoprolol; Receptors, Adrenergic, beta-1; Receptors, Adrenergic, beta-2; Time Factors
PubMed: 8227468
DOI: 10.1002/j.1552-4604.1993.tb01930.x -
Clinical Cardiology Feb 1983
Topics: Acebutolol; Adult; Arrhythmias, Cardiac; Blood Pressure; Drug Evaluation; Electrocardiography; Female; Heart Rate; Heart Ventricles; Humans; Male; Middle Aged
PubMed: 6831786
DOI: 10.1002/clc.4960060204 -
Journal of Clinical Pharmacology May 1988Acebutolol, a beta-1 selective beta blocker with intrinsic sympathomimetic activity has been shown to be an effective agent in chronic angina pectoris therapy, with... (Clinical Trial)
Clinical Trial
Acebutolol, a beta-1 selective beta blocker with intrinsic sympathomimetic activity has been shown to be an effective agent in chronic angina pectoris therapy, with twice or three times daily dosing. The long-term effects of 400 mg of acebutolol given only once a day versus placebo on exercise hemodynamics, ST segment depression, and rate pressure product were studied. Eleven patients (mean age, 60 +/- 12 years) with hypertension and chronic angina pectoris were enrolled. Resting heart rate was not significantly altered after therapy, (80 vs 72 bpm). Objective measurements from exercise treadmill tests showed significant reduction in peak heart rate from 130 to 103 bpm, systolic blood pressure from 197 to 167 mm Hg, rate pressure product (from 25 to 18 bpm-mm Hg X 1000), and ST depression in patients receiving acebutolol compared with those receiving placebo. No significant adverse effects were reported. These data indicate that acebutolol may be efficacious as once daily therapy for chronic stable angina pectoris.
Topics: Acebutolol; Adult; Aged; Aged, 80 and over; Angina Pectoris; Electrocardiography; Female; Humans; Hypertension; Male; Middle Aged; Physical Exertion
PubMed: 3392240
DOI: 10.1002/j.1552-4604.1988.tb05754.x -
Farmakologiia I Toksikologiia 1991Thirty-two patients with hypertensive disease were treated with a cardioselective blocker of beta-adrenergic receptors acebutolol ("Sectral-400", Rhone Poulenc, France)....
Thirty-two patients with hypertensive disease were treated with a cardioselective blocker of beta-adrenergic receptors acebutolol ("Sectral-400", Rhone Poulenc, France). The binding of the drug and its metabolites diacetolol to plasma proteins and erythrocytes and their excretion with the saliva were studied. The significant binding of acebutolol and diacetolol to erythrocytes was shown. The ratio of the content of the free form of these substances in erythrocytes to plasma content was on the average 1.54 +/- 0.96 for diacetolol and 1.93 +/- 1.01 for acebutolol. A good correlation of acebutolol and diacetolol contents in the saliva with their contents in plasma was found. The mean values of the protein-bound fraction were for acebutolol 0.133 +/- 0.038 and for diacetolol 0.106 +/- 0.050.
Topics: Acebutolol; Adult; Blood Proteins; Chromatography, High Pressure Liquid; Erythrocytes; Humans; Hypertension; Middle Aged; Protein Binding; Saliva; Time Factors
PubMed: 1860501
DOI: No ID Found -
La Nouvelle Presse Medicale Nov 1982
Topics: Acebutolol; Adult; Female; Humans; Male
PubMed: 7155871
DOI: No ID Found -
The American Journal of Cardiology Aug 1990Acebutolol et Prévention Secondaire de l'Infarctus (APSI), a randomized, placebo-controlled trial, was designed to test long-term acebutolol, 200 mg twice daily, a beta... (Clinical Trial)
Clinical Trial Randomized Controlled Trial
Acebutolol et Prévention Secondaire de l'Infarctus (APSI), a randomized, placebo-controlled trial, was designed to test long-term acebutolol, 200 mg twice daily, a beta blocker with mild intrinsic sympathomimetic activity, in the prevention of late death in high-risk postacute myocardial infarction (AMI) patients. APSI was planned because patients with a death rate greater than 20% have not been enrolled in significant numbers in previous trials and in such high-risk patients, it remained to be proven that beta blockers have a beneficial effect. Patients with an expected average risk of greater than 20% were to be selected based on clinical criteria. At the time of the second interim analysis, the placebo group 1-year mortality was much lower than expected (12%). The ethical board recommended to stop the trial: 309 patients had been allocated to placebo, 298 to acebutolol. The average delay between onset of symptoms and inclusion was 10.5 days. The average follow-up was 318 days after inclusion. About the same number of patients were discontinued from study treatment in both groups. All patients were included in the analysis. There were 17 deaths in the acebutolol group and 34 in the placebo group, a 48% decrease (p = 0.019). The vascular mortality decreased by 58% (p = 0.006), the highest ever observed with a beta blocker. All cardiovascular causes of death, including congestive heart failure, were less frequent in the acebutolol group. Although the objective was not achieved, APSI patients were at a higher risk than the average of the 9 previous trials with beta blockers (12% instead of 7%). In addition, the total mortality reduction did not decrease in 9 subgroups with increasing mortality risk from 2 to 23%. APSI shows that moderately severe postAMI patients can benefit from a beta-blocking treatment and a beta-blocker with mild intrinsic sympathomimetic activity can be effective.
Topics: Acebutolol; Administration, Oral; Aged; Female; Follow-Up Studies; Humans; Male; Middle Aged; Multicenter Studies as Topic; Myocardial Infarction; Randomized Controlled Trials as Topic; Risk Factors; Statistics as Topic; Survival Rate
PubMed: 2195860
DOI: 10.1016/0002-9149(90)90831-k -
La Nouvelle Presse Medicale Dec 1975
Topics: Acebutolol; Blood Pressure; Drug Tolerance; Heart Rate; Humans; Hypertension
PubMed: 1219636
DOI: No ID Found -
Archives of Pharmacal Research Jun 2003Because physiological changes that potentially alter pharmacokinetics occurs in diabetes mellitus patients, pharamacokinetics of drugs used in the treatment of... (Comparative Study)
Comparative Study
Because physiological changes that potentially alter pharmacokinetics occurs in diabetes mellitus patients, pharamacokinetics of drugs used in the treatment of hypertension was studied using acebutolol as a model anti-hypertensive drug. Thus, the pharmacokinetics of acebutolol was investigated after oral administration of acebutolol (15 mg/kg) to control rabbits and rabbits with acute or chronic diabetes mellitus induced by alloxan. Kidney and liver functions were documented for acute and chronic diabetes mellitus groups based on plasma chemistry data. After oral administration of acebutolol to acute and chronic groups, the plasma concentrations appeared higher; As a result, area under the plasma concentration-time curve from time zero to time infinity10575 and 8668 microg x h/mL for acute and chronic group, respectively. In comparison, the area was apparently smaller in the control group (i.e., 7132 microg x h/mL). The half-life in acute groups was significantly prolonged 8.45 h compared with the half-life in the control group (i.e., 6.30 h). Alteration in acebutolol pharmacokinetics was more pronounced in the acute group as evidenced by the significantly higher values the area under the plasma concentration time curve, absorption rate constant and maximum plasma concentration compared with chronic or control group. Therefore, these observations indicate that acebutolol pharmacokinetics may be affected in patients with diabetes mellitus, especially in the early stage of the disease.
Topics: Acebutolol; Administration, Oral; Animals; Diabetes Mellitus, Experimental; Rabbits
PubMed: 12877562
DOI: 10.1007/BF02976870 -
Current Medical Research and Opinion 1980Propranolol has recently been shown to produce some impairment of psychomotor performance in human volunteers. This beta-blocking compound, however, is lipophilic and... (Clinical Trial)
Clinical Trial Comparative Study Randomized Controlled Trial
Propranolol has recently been shown to produce some impairment of psychomotor performance in human volunteers. This beta-blocking compound, however, is lipophilic and readily penetrates the blood-brain barrier to gain access to the central nervous system. Acebutolol has a lower lipid solubility. A study was carried out, therefore, to compare the psychomotor effect of the two beta-blocking drugs. Any subjectively experienced side-effects were also recorded. Ten healthy volunteers were given single doses of 40 mg propranolol, 100 mg acebutolol and placebo on a random double-blind basis and the effect, if any, on performance was measured using a particularly sensitive complex reaction time technique. Propranolol produced a significant prolongation of complex reaction time when compared with placebo or acebutolol. Acebutolol did not significantly increase complex reaction time over the placebo value. Two subjects reported mild feelings of 'muzziness' after taking propranolol. No side-effects were reported after acebutolol.
Topics: Acebutolol; Adult; Double-Blind Method; Humans; Male; Motor Skills; Propranolol
PubMed: 7428410
DOI: 10.1185/03007998009116512