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PubMedDate not supplied

Effects of equipotent blocking doses of acebutolol, acebutolol's primary metabolite, and propranolol on left ventricular hemodynamics in conscious awake dogs.

In six conscious dogs we compared the hemodynamic effects of propranolol, acebutolol, and acebutolol's primary metabolite at equipotent beta-blocking doses. Aortic pressure, heart rate, left ventricular end-diastolic pressure, dP/dt, and aortic flow velocity were measured 3 weeks after sterile surgery during three infusions of each drug. Only one drug was given on each day. The equipotent beta-blocking dose of each drug was obtained by comparing isoproterenol dose-response curves. All three drugs produced a fall in dP/dt. Left ventricular end-diastolic pressure increased in most dogs, but this was only significant for acebutolol. The heart rate tended to fall and the blood pressure rise, but this was variable and not significant. The concentration of the equipotent blocking dose of acebutolol was 44 times that of propranolol, and while the concentration of acebutolol's metabolite was 1.6 times that of acebutolol. In conclusion, at a concentration similar to acebutolol, acebutolol's metabolite has heart rate blocking and myocardial depressive effects similar to those of propranolol and acebutolol.

Acebutolol↗
PubMed2002

Pharmacokinetics of acebutolol and its main metabolite, diacetolol after oral administration of acebutolol in rabbits with carbon tetrachloride-induced hepatic failure.

Pharmacokinetic characteristics of acebutolol and its main metabolite, diacetolol, following a single 10 mg/kg oral dose, were investigated in rabbits with carbon tetrachloride-induced hepatic failure. Plasma concentrations of acebutolol and diacetolol were determined by a high performance liquid chromatography assay. The area under the plasma concentration-time curves (AUC) and maximum plasma concentration (Cmax) of acebutolol were significantly increased in moderate and severe carbon tetrachloride-induced hepatic failure rabbits. The ratio of the diacetolol to total acebutolol in plasma (i.e., metabolite percentage rate) was significantly decreased in moderate and severe carbon tetrachloride-induced hepatic failure rabbits. Volume of distribution (Vd) and total body clearance (CL1) of acebutolol were significantly decreased in moderate and severe carbon tetrachloride-induced hepatic failure rabbits. Slope of terminal phase (beta) of acebutolol was significantly decreased in hepatic failure rabbits. These findings suggest that the Vd, CL1 and beta of acebutolol were significantly decreased as a result of inhibition of the hepatic metabolism in moderate to severe hepatic failure rabbits. Therefore, dose adjustment may be necessary for acebutolol in hypertensive patients with hepatic damage.

Acebutolol↗
PubMed1977

[Biochemical studies of acebutolol-the beta1 specificity of acebutolol (author's transl)].

Effects of acebutolol on carbohydrate and lipid metabolism in rats and on adenylate cyclase of heart and liver in dogs were investigated to determine the beta receptor blocking properties of the compound. Acebutolol exhibited the beta blocking activity and inhibited the increase of serum lactate concentration induced by adrenaline. This inhibition was about one-sixth as potent as that of propranolol. In hyperglycemic and free fatty acid effects of adrenaline, acebutolol inhibited the adrenaline-induced free fatty acid increase more effectively than hyperglycemia induced by adrenaline. In the inhibition of stimulated adenylate cyclase activity in the heart and liver, acebutolol was more active on the heart than on liver. Relative beta1 specificity of acebutolol was 93.2. Inhibition of propranolol on adenylate cyclase activity was more potent than that of acebutolol on both tissues, but showed no specificity. These results suggest that acebutolol is beta1 selective, although its beta blocking potency is less than that of propranolol.

Acebutolol↗
PubMedDate not supplied

The pharmacokinetics of acebutolol in man, following the oral administration of acebutolol HCl as a single dose (400 mg), and during and after repeated oral dosing (400 mg, b.d.).

The pharmacokinetics of acebutolol have been studied in eight healthy male volunteers following the oral administration of acebutolol hydrochloride ('Sectral', May & Baker) as a single dose (400 mg), and during and after repeated oral dosing (400 mg, b.d. for 56 days). Following single dose administration, considerable inter-subject variation in plasma levels of parent drug and the major metabolite, diacetolol, was evident. Acebutolol appeared to be eliminated from plasma in a bi-phasic manner, and this was confirmed from urinary excretion rate data. Mean initial and terminal half-lives of about 2 and 11 h, respectively, were determined. Plasma levels of diacetolol were greater than those of parent drug from 3 to 4 h following dose administration. Total urinary excretion of diacetolol was generally greater than that of acebutolol. During repeated dosing, steady-state plasma levels of acebutolol and diacetolol were achieved in 6 volunteers. Acebutolol did not appear to stimulate or inhibit its metabolism.

Acebutolol↗
PubMed1997

Persistent reduction of mortality for five years after one year of acebutolol treatment initiated during acute myocardial infarction. The APSI Investigators. Acebutolol et Prévention Secondaire de l'Infarctus.

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 < 0.01) only for the first year and was not significantly different thereafter. Thus, the initial benefit obtained in 1 year of treatment by acebutolol lasts for 5 years.

Acebutolol↗
PubMed1985

Effects of a fixed combination of low dose nifedipine and acebutolol on essential hypertension: comparison with standard dose acebutolol.

114 patients from four clinics participated in a double blind study designed to assess the efficacy of a nifedipine-acebutolol fixed combination -10 mg + 100 mg - as compared with acebutolol -200 mg- in essential hypertension. During the ten week study the mean blood pressure readings (s.d.) 1-3 h after treatment decreased from 179.2/104.8 (10.2/6.2) to 150.3/87.7 (9.8/7.7) in the combination group and from 181.7/106.5 (14.4/7.0) to 150.4/89.0 (15.0/10.4) in the acebutolol group. The mean systolic and diastolic blood pressures were also decreased after exertion (load) and 24 hours after treatment at the end of the 6th week of the study. A doubling of the dose from week 7 to 10 did not change these figures. These results reveal the possibility of treating essential hypertension with a low dose of beta-adrenergic blocking agents in combination with 10 mg nifedipine. Both drugs were well tolerated. 3 patients (5%) in the combination group and 3 patients in the acebutolol group were withdrawn from the study because of headache and dizziness.

Acebutolol↗
PubMedDate not supplied

Acebutolol (400 mg) given as a single daily dose to hypertensive patients previously stabilized on 400 mg acebutolol daily in divided doses: an open multicentre study.

An open multicentre trial was carried out in 13 hypertensive patients, who had responded satisfactorily to and been stabilized on treatment with 400 mg acebutolol daily in divided doses, to assess the effectiveness and tolerance of the same daily dosage given as a single morning dose. On admission, patients were changed over immediately to the new dosage regimen and continued on it for 3 months. Blood pressure and pulse rate measurements were made on the day before change over and then at the end of each month. The results indicated that once-a-day 400 mg acebutolol gave satisfactory continued control of blood pressure. Side-effects reported spontaneously by the patient, observed by the physician, and elicited in response to a questionnaire, diminished in incidence and severity in most of the patients during the trial period.

Acebutolol↗
PubMed1985

Acebutolol in essential hypertension: results of two multicenter studies against placebo and propranolol.

Two double-blind multicenter studies compared acebutolol with placebo (acebutolol, N = 121; placebo, N = 116) and with propranolol (acebutolol, N = 186; propranolol, N = 190) in essential hypertension. Acebutolol significantly reduced mean sitting diastolic blood pressure from 99.2 +/- 0.3 mm Hg at baseline to 89.1 +/- 0.9 mm Hg at the end of dose titration (p = 0.001). Significantly more acebutolol patients (65%) achieved therapeutic goal than did placebo patients (28%, p less than 0.01). The reduction in heart rate in acebutolol-treated patients (9.2 bpm) was greater than in placebo-treated patients (1.2 bpm, p = 0.001). The incidence of side effects and the number of patients discontinued because of side effects did not significantly differ between acebutolol and placebo. Acebutolol and propranolol produced comparable reductions in diastolic, systolic, and mean arterial blood pressures (p less than 0.001). At equipotent doses the 13% decrease in heart rate in patients receiving acebutolol was significantly less than the 17% decrease in propranolol patients (p = 0.02). The number of patients experiencing central nervous system (CNS) side effects while receiving acebutolol (N = 50) was significantly less than with propranolol (N = 75, p = 0.001), and significantly fewer acebutolol patients (N = 11) were discontinued because of side effects compared with propranolol patients (N = 29, p less than 0.01). Laboratory, ECG, or chest X-ray results did not differ for acebutolol, placebo, or propranolol. Acebutolol appears to be safe and effective in the management of mild to moderately severe essential hypertension and is better tolerated than propranolol in terms of CNS side effects, with a significantly lesser effect on heart rate.

Acebutolol↗
PubMed1991

A comparative pharmacokinetic and pharmacodynamic study of conventional and sustained-release preparations of acebutolol in healthy volunteers.

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.

Acebutolol↗
PubMed1982

Favorable effects of acebutolol on exercise performance and angina in men with coronary artery disease.

Acebutolol, a relatively cardioselective beta-adrenergic blocking drug, was administered to 20 men with coronary artery disease and angina. A three month double-blind cross-over (placebo and acebutolol) design was used following a 12-week placebo phase and a six-week dose-titration phase. During the cross-over phase, acebutolol (400 mg in 19 men and 300 mg in one, orally three times per day) increased the duration of treadmill exercise (placebo, 6.8 +/- 0.5) min [average +/- SEM]; acebutolol, 8.1 +/- 0.6 min; P less than 0.05) and decreased the frequency of ST segment depression during exercise (placebo, 12 or 20 men; acebutolol, 6 of 20 men). The heart rate x systolic blood pressure product (x 10(-2)) was decreased both at rest (placebo, 105.0 +/- 4.0; acebutolol, 84.0 +/- 3.0; P less than 0.01) and during exercise (placebo, 199.0 +/- 10.0; acebutolol, 144.0 +/- 8.0; P less than 0.01). Acebutolol treatment decreased the frequency of angina (diary cards) (placebo, 9.0 +/- 2.4 episodes per week; acebutolol, 6.4 +/- 2.2 episodes per week; P less than 0.05) and decreased the consumption of nitroglycerin (placebo, 9.0 +/- 4.4 tablets per week; acebutolol, 7.4 +/- 4.0 tablets per week; P less than 0.05). Results suggest that acebutolol increases exercise performance and decreases the occurrence of angina in men with coronary disease.

Acebutolol↗
PubMed1986

The effects of acebutolol alone and in combination with furosemide or hydralazine in experimentally induced hypertensive G-minipigs.

Experimentally induced hypertensive G-minipigs were used for assessing the antihypertensive effects of acebutolol, a cardioselective beta-adrenergic blocking agent. In the acute experiment, six females were used. Acebutolol (3 mg/kg, i.v.) alone or in combination with furosemide (1 mg/kg, i.v.) or hydralazine (1 mg/kg, i.v.) was administered through an implanted catheter. In the chronic experiments, five females received oral acebutolol (100-200 mg/day). The blood pressure, heart rate, plasma renin activity (PRA) and plasma aldosterone concentration (PAC) were used as parameters. In the acute experiment, there were no marked changes in the blood pressure or heart rate during the nondosing period. Acebutolol alone caused a marked decrease in the blood pressure and heart rate. In the two combination tests, combined administration with acebutolol and furosemide had a greater effect on the blood pressure and heart rate than did acebutolol alone. A combined acebutolol and hydralazine regimen caused a slight reduction not only in the blood pressure, but also in the heart rate compared with acebutolol alone. PRA and PAC remained essentially constant, with minor fluctuations, throughout the nondosing period. Following the injection of acebutolol alone, PRA showed an elevation with a significant rise after three hours and PAC showed a tendency to increase. PRA and PAC generally tended to increase in the case of combined administration with furosemide or hydralazine, but these tendencies were less conspicuous than with acebutolol alone. On the other hand, chronic treatment with acebutolol produced a significant decrease in the heart rate from two weeks after the administration and in the blood pressure from four weeks.(ABSTRACT TRUNCATED AT 250 WORDS)

Acebutolol↗
PubMed1985

Comparison of acebutolol and propranolol in essential hypertension.

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.

Acebutolol↗
PubMed1983

Effects of acebutolol on paroxysmal atrioventricular reentrant tachycardia in patients with manifest or concealed accessory pathways.

Electrophysiologic studies before and after administration of 50 mg of intravenous (IV) acebutolol were performed in 20 patients. Four of the 20 had persistent preexcitation, two had intermittent preexcitation, and 14 had a concealed retrogradely conducting accessory pathway (AP). Acebutolol depressed anterograde AP conduction with loss of preexcitation in one patient and increased the effective refractory period of AP in the remaining three; in most, it depressed anterograde normal pathway conduction. The longest atrial paced cycle length producing atrioventricular (AV) nodal block increased from 290 +/- 7 to 39 +/- 6 msec (mean +/- SEM) after acebutolol (p less than 0.01). Acebutolol had no significant effect on retrograde AP conduction. Sustained AV reentrant tachycardia was inducible in all 20 patients before acebutolol and in 19 after acebutolol. The cycle length of tachycardia increased from 323 +/- 8 to 352 +/- 8 msec after acebutolol (p less than 0.01), reflecting an increment of A-H interval from 148 +/- 8 to 174 +/- 9 msec (p less than 0.01). Electrophysiologic studies were reported after 800 mg of oral acebutolol given in four divided doses at six-hour intervals in eight patients. The results were comparable to those of IV acebutolol. Thus, acebutolol depresses AV nodal conduction and slows the rate of AV reentrant tachycardia, but is generally ineffective in inhibiting the induction of sustained tachycardia. It occasionally depresses anterograde AP conduction.

Acebutolol↗
PubMed1975

[Pharmacokinetics of acebutolol].

Pharmacodynamic data correlating beta-adrenoceptor blockade with plasma level of drug were obtained in healthy male volunteers (3). Direct comparison of the inhibition of isoprenaline induced tachycardia was achieved in each volunteer after the administration of single doses of either acebutolol (300 mg), practolol (400 mg) or propranolol (40 mg). These drugs were approximately equipotent at these doses, at the times of maximum beta-adrenoceptor blockade. Pharmacokinetic data were obtained in hypertensive male patients (4) after treatment with 14C-radioactively labelled acebutolol hydrochloride. Both 'total-14C' levels and specific '14C-acebutol' levels were determined in plasma, urine and faeces. It was shown, by calculation from the renal clearance, that the late biological half-life for the decline of 14C-acebutolol in plasma was 9.4 h and 13.2 h, respectively, in two of these patients treated with a single oral dose (200 mg) of 14C-acebutolol hydrochloride. In one of the patients treated by intravenous infusion (20 mg/10 mn), the late biological half-life plasma was calculated to be 7.5 h. Renal clearance of acebutolol was shown to be close to a mean of 83 ml plasma/mn for each of three patients (two oral and one intravenous) in spite of the fact that one of the orally treated patients had an elevated level of urea in his plasma (47 mg/100 ml) indicative of some impairment of kidney function. The recovery of 14C-radioactivity in the urine (29 p. cent) and faeces (64 p. cent) was 93 p.cent of the dose of labelled acebutolol in one of the orally treated patients. The overall proportion of the dose excreted as unchanged 14C-acebutolol was 62 p.cent. The major metabolite was the product formed by shortening of the butyramido-group of acebutolol to form an acetamido-group. This metabolite was also readily excreted in both urine and faeces and was also detected in an extract of the 4 h plasma from an orally treated patient. It was identified by co-chromatography as the acetyl analogue (M & B 16 942) of acebutolol. It would be detected by the colorimetric assay of acebutolol in plasma because the same aromatic amino-compound (M & B 17 127) would be formed during the acid hydrolysis procedure. A small quantity of an other unidentified metabolite was detected in an extract of freeze-dried urine after autoradiography of a two dimensional thin layer silica-gel chromatogram.

Acebutolol↗
PubMed1985

Once-daily acebutolol and atenolol in essential hypertension: double-blind crossover comparison.

Acebutolol was compared to atenolol in 33 patients with mild to moderate essential hypertension (diastolic blood pressure greater than 95 mm Hg) with the use of a double-blind crossover study design. At 8 weeks of treatment, acebutolol, 400 mg once daily, and atenolol, 100 mg once daily, produced similar significant (p less than 0.01) reductions in average mean arterial blood pressure (12% and 11%, respectively) from baseline. Average heart rate at 4 weeks was also significantly reduced (p less than 0.01) from baseline (acebutolol, 14.8%; atenolol, 18.3%); the reduction with acebutolol, however, was significantly less (p less than 0.05) than that seen with atenolol. Both agents produced similar effects during exercise, and serum drug determinations showed acebutolol to be rapidly metabolized. Acebutolol appeared to be better tolerated: the frequency of side effects with acebutolol (24%) was less than with atenolol (45%). Acebutolol is as effective as atenolol in mild to moderate essential hypertension. Acebutolol appears to be better tolerated and to have a lesser effect on heart rate than atenolol.

Acebutolol↗