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British Journal of Clinical Pharmacology Sep 19811 Nine hypertensive patients received by mouth daily doses of 400 mg of acebutolol and then, after a 2 week washout period, 80 mg of propranolol for 2 week periods in an...
1 Nine hypertensive patients received by mouth daily doses of 400 mg of acebutolol and then, after a 2 week washout period, 80 mg of propranolol for 2 week periods in an open study. 2 Both treatments caused equivalent cardiac blockade as assessed by reduction in exercise tachycardia. 3 Both treatments lowered blood pressure, although this effect on pressure was better maintained in the case of acebutolol. 4 Forearm blood flow, at rest, was significantly reduced at 2 h after dosing with propranolol, but not after acebutolol. 5 This difference between the two drugs is probably due to the cardioselectivity of orally administered acebutolol in man.
Topics: Acebutolol; Administration, Oral; Adult; Blood Pressure; Female; Forearm; Heart Rate; Humans; Hypertension; Male; Middle Aged; Physical Exertion; Propranolol; Regional Blood Flow; Vascular Resistance
PubMed: 7295466
DOI: 10.1111/j.1365-2125.1981.tb01227.x -
The Journal of International Medical... 1978Acebutolol (Sectral) was used successfully in a clinical trial involving thirty-two hypertensive patients. Twenty-three patients received acebutolol at a dosage of... (Clinical Trial)
Clinical Trial Comparative Study
Acebutolol (Sectral) was used successfully in a clinical trial involving thirty-two hypertensive patients. Twenty-three patients received acebutolol at a dosage of 400--800 mg daily as sole treatment and nine patients received concurrent treatment with thiazide diuretics. In both groups of patients there was a substantial fall in diastolic and systolic pressure to levels within the normotensive range. The combination of acebutolol with thiazide diuretics was a particularly effective form of anti-hypertensive treatment where a greater anti-hypertensive effect was required. Acebutolol did not significantly slow the heart rate. The only side-effect was slight pitting oedema of both legs in one patient. Acebutolol appears to be a useful anti-hypertensive in the management of hypertension.
Topics: Acebutolol; Adult; Aged; Benzothiadiazines; Clinical Trials as Topic; Diuretics; Drug Therapy, Combination; Female; Heart Rate; Humans; Hypertension; Male; Middle Aged; Pulse; Sodium Chloride Symporter Inhibitors
PubMed: 342303
DOI: 10.1177/030006057800600112 -
Headache Mar 1978
Clinical Trial Comparative Study
Topics: Acebutolol; Clinical Trials as Topic; Humans; Migraine Disorders
PubMed: 348644
DOI: 10.1111/j.1526-4610.1978.hed1801020.x -
British Journal of Clinical Pharmacology Dec 2005We aimed to investigate effects of grapefruit juice on acebutolol pharmacokinetics. (Randomized Controlled Trial)
Randomized Controlled Trial
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 (AUC(0-33 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, AUC(0-33 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.
Topics: Acebutolol; Adrenergic beta-Antagonists; Adult; Anti-Arrhythmia Agents; Antihypertensive Agents; Beverages; Citrus paradisi; Cross-Over Studies; Female; Food-Drug Interactions; Hemodynamics; Humans; Male
PubMed: 16305592
DOI: 10.1111/j.1365-2125.2005.02489.x -
Clinical Pharmacology and Therapeutics Jul 1980A double-blind, randomized study comparing the efficacy of intravenous acebutolol with propranolol on frequent premature ventricular complexes (PVCs) in 24 patients is... (Clinical Trial)
Clinical Trial Comparative Study Randomized Controlled Trial
A double-blind, randomized study comparing the efficacy of intravenous acebutolol with propranolol on frequent premature ventricular complexes (PVCs) in 24 patients is reported. Frequent PVCs were abolished or reduced by 75% or more in 10 of 12 patients (83%) given acebutolol and in 10 of 12 patients (83%) given propranolol. The therapeutic effect of acebutolol lasted for at least 1 hr in 4 of 12 patients (33%), for at least 3.5 hr in 3 of 12 patients (25%), and for at least 4 hr in 2 of 12 patients (17%). The effect of propranolol lasted for at least 1 hr in 6 of 12 patients (50%), for at least 3.5 hr in 4 of 12 patients (33%), and for at least 4 hr in 4 of 12 patients (33%). Hence, intravenous acebutolol and propranolol were equally effective.
Topics: Acebutolol; Aged; Arrhythmias, Cardiac; Clinical Trials as Topic; Double-Blind Method; Female; Heart Rate; Humans; Injections, Intravenous; Male; Middle Aged; Propranolol; Random Allocation; Time Factors
PubMed: 6993085
DOI: 10.1038/clpt.1980.126 -
Drugs 1988
Topics: Acebutolol; Arteriosclerosis; Humans
PubMed: 3215127
DOI: No ID Found -
British Journal of Clinical Pharmacology Mar 19811 The acute cardiovascular effects of acebutolol were measured at constant paced heart rate in thirteen patients investigated for possible coronary artery disease, six...
1 The acute cardiovascular effects of acebutolol were measured at constant paced heart rate in thirteen patients investigated for possible coronary artery disease, six of whom showed significant coronary stenosis with regional myocardial dysfunction, seven of whom proved normal. Acebutolol 0.75 mg/kg i.v. was given to three patients with coronary artery disease and three normals, and 1 mg/kg i.v. to the other patients.2 Measurements were made of cardiac output, left ventricular and arterial pressures, and left ventricular angiography. Isovolumic and ejection phase parameters of left ventricular function, and systemic vascular resistance were derived. Plasma levels of acebutolol were measured. 3 The acute effects of acebutolol were a slight fall in cardiac output, LV dp/dt and dP/dt/P. There was no change in LV or arterial pressures, no consistent change in LVEDP or EDV, and no consistent change in ejection fraction or mean VCF. These changes imply a small negative inotropic effect, more marked at the higher dose. 4 The effects of acebutolol differed in patients with ischaemic heart disease compared with normals in that LVEDP and EDV increased, mean VCF decreased and cardiac output was lowered more. 5 These data are consistent with myocardial and vascular effects of beta-adrenoceptor blockade more marked at the higher dose and more marked in patients with ischaemic heart disease.
Topics: Acebutolol; Adult; Aged; Blood Pressure; Cardiac Output; Coronary Disease; Female; Heart Rate; Hemodynamics; Humans; Male; Middle Aged; Vascular Resistance
PubMed: 7213527
DOI: 10.1111/j.1365-2125.1981.tb00532.x -
British Journal of Clinical Pharmacology Feb 1980
Topics: Acebutolol; Adult; Humans; Injections, Intravenous; Kinetics; Male; Middle Aged
PubMed: 7356910
DOI: 10.1111/j.1365-2125.1980.tb05837.x -
American Heart Journal May 1985Acebutolol, a new beta-blocking agent, possesses the ancillary pharmacologic properties of cardioselectivity and partial agonist and membrane-stabilizing activities....
Acebutolol, a new beta-blocking agent, possesses the ancillary pharmacologic properties of cardioselectivity and partial agonist and membrane-stabilizing activities. Compared to propranolol at equipotent doses, acebutolol produces less bronchoconstriction and preserves the bronchodilator response to isoprenaline. Similarly, acebutolol has less of an effect on peripheral vascular hemodynamics than does propranolol. Because of partial agonist activity, acebutolol produces a lesser reduction in heart rate and cardiac output than do propranolol and atenolol and has been found to have minimal effects on lipoprotein metabolism. Acebutolol may be the only beta-blocking agent that demonstrates some membrane-stabilizing activity at clinically achievable plasma concentrations. The ancillary pharmacologic properties of cardioselectivity and partial agonist activity are distinct and offer definite advantages to selected patients, particularly patients with respiratory disease, in whom cardioselective acebutolol, particularly at low doses, can minimize patient risk. The ancillary property of membrane-stabilizing activity may also guide therapy in selected patients.
Topics: Acebutolol; Adrenergic beta-Agonists; Adrenergic beta-Antagonists; Asthma; Bronchi; Cell Membrane; Heart; Humans; Hypertension; Pulmonary Ventilation; Vital Capacity
PubMed: 2859777
DOI: 10.1016/0002-8703(85)90698-2 -
The American Journal of Cardiology Sep 1979To evaluate the antiarrhythmic efficacy of the new beta adrenergic blocking agent acebutolol, 15 monitored patients with supraventricular arrhythmias received, in... (Clinical Trial)
Clinical Trial
To evaluate the antiarrhythmic efficacy of the new beta adrenergic blocking agent acebutolol, 15 monitored patients with supraventricular arrhythmias received, in double-blind fashion, an intravenous infusion of either acebutolol or saline solution after a control period. Patients treated with saline solution demonstrated no change (P greater than 0.05) in heart rate or arterial blood pressure or conversion to sinus rhythm. After administration of acebutolol, significant (P less than 0.05) reductions in heart rate were noted at 5 minutes. Peak reduction occurred at 10 to 30 minutes and correlated with maximal acebutolol plasma concentrations, antiarrhythmic activity persisted for 24 hours. Mild reductions in systolic blood pressure were observed in the majority of patients. Two patients with atrial fibrillation and one with multifocal atrial tachycardia had conversion to sinus rhythm. Frequent premature atrial complexes noted in one patient were greatly suppressed after administration of the drug. In the nine patients with clinical evidence of chronic obstructive lung disease acebutolol was well tolerated. Adverse reactions were limited to transient dyspnea in one patient with prior heart failure and a decrease in systolic blood pressure to less than 90 mm Hg in three patients who remained asymptomatic. In the patients studied, acebutolol was an effective agent for the treatment of supraventricular arrhythmias and appeared to be of special value in those with chronic obstructive lung disease.
Topics: Acebutolol; Adult; Aged; Arrhythmias, Cardiac; Blood Pressure; Clinical Trials as Topic; Double-Blind Method; Female; Heart Failure; Heart Rate; Humans; Male; Middle Aged; Respiratory Function Tests; Sodium Chloride
PubMed: 382821
DOI: 10.1016/0002-9149(79)90406-5