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American Heart Journal May 1985During 10 years of clinical use involving almost 3 million patient-years, acebutolol has become established as a remarkably safe and well-tolerated beta-blocking agent,... (Review)
Review
During 10 years of clinical use involving almost 3 million patient-years, acebutolol has become established as a remarkably safe and well-tolerated beta-blocking agent, effective in treating essential hypertension and cardiac arrhythmias. The existence of a long-lived active metabolite (diacetolol) confers a 24-hour duration of action, which permits effective use of a once-daily regimen, particularly for hypertension. Acebutolol has low lipid solubility and low protein binding; the former property reduces the risk of central side effects, and the latter means that displacement interactions with other drugs are unlikely. Because acebutolol and its metabolite normally have both renal and hepatic excretion pathways, an alternative pathway is available should either be compromised through disease. Acebutolol is cardioselective, and clinical use has borne out the low incidence of bronchospasm in patients with impaired lung function. The possession of intrinsic sympathomimetic activity (ISA) leads to only modest reductions in cardiac output, which in turn reduces the chance of excessive bradycardia and the likelihood of precipitating heart failure. A combination of selectivity and ISA may be responsible for the low incidence of tiredness and cold extremities observed with acebutolol compared with other beta blockers. The unique pharmacologic and pharmacokinetic profile of acebutolol confers several therapeutic advantages and may be responsible for the generally low level of side effects experienced in clinical use.
Topics: Acebutolol; Adrenergic beta-Antagonists; Age Factors; Animals; Arrhythmias, Cardiac; Blood Circulation; Bronchi; Chemical Phenomena; Chemistry; Drug Interactions; Humans; Hypertension; Kidney Diseases; Kinetics; Liver Diseases; Sympathomimetics
PubMed: 2859785
DOI: 10.1016/0002-8703(85)90712-4 -
Pharmacotherapy 1986Acebutolol is a new hydrophilic, cardioselective beta-adrenergic-blocking agent that possesses partial agonist and membrane-stabilizing activities. In the treatment of... (Review)
Review
Acebutolol is a new hydrophilic, cardioselective beta-adrenergic-blocking agent that possesses partial agonist and membrane-stabilizing activities. In the treatment of mild to moderate essential hypertension, once-daily acebutolol as monotherapy provides effective control in a large majority of patients and produces a further reduction in blood pressure when used concomitantly with diuretics. Acebutolol is as effective as other beta-blocking agents, and in a large, double-blind, parallel study against propranolol was found to cause less reduction in heart rate, and fewer neurologic side effects and patient withdrawals due to adverse effects. Oral acebutolol is also effective in suppressing premature ventricular contractions, and in small numbers of patients generally beneficial results were obtained in supraventricular and ventricular arrhythmias with intravenous administration. These salutary effects are attributable to beta blockade. Controlled clinical trials documented the antianginal actions of oral acebutolol in chronic stable angina pectoris; its efficacy in this regard is comparable to that of other beta-blocking agents. The drug produces smaller decreases in heart rate and cardiac output and alterations in peripheral vascular hemodynamics than beta-blocking drugs without partial agonist activity, and because of its cardioselectivity, it may be used cautiously in patients with bronchospastic disease. Acebutolol has minimal metabolic effects and does not elevate levels of blood lipids during long-term therapy; high-density-lipoprotein cholesterol increased with acebutolol in a small number of patients.
Topics: Acebutolol; Angina Pectoris; Animals; Arrhythmias, Cardiac; Central Nervous System; Drug Administration Schedule; Drug Interactions; Heart; Heart Conduction System; Hemodynamics; Humans; Hypertension; Kinetics; Myocardial Contraction; Receptors, Adrenergic, beta; Respiration
PubMed: 3012486
DOI: 10.1002/j.1875-9114.1986.tb03451.x -
Drugs Jun 1985Acebutolol is a cardioselective beta-adrenoceptor blocking drug possessing both partial agonist (intrinsic sympathomimetic) and membrane stabilising activity. In... (Review)
Review
Acebutolol is a cardioselective beta-adrenoceptor blocking drug possessing both partial agonist (intrinsic sympathomimetic) and membrane stabilising activity. In hypertension, it can be administered once or twice daily with equal effectiveness, and has been as effective at lowering blood pressure as propranolol, diuretics, and other beta-blocking drugs (metoprolol, labetalol and atenolol) and more effective than methyldopa. Acebutolol has a significantly smaller effect on resting heart rate than propranolol, metoprolol and atenolol, although direct comparisons with drugs with intrinsic sympathomimetic activity have yet to be undertaken. In both angina and arrhythmia, when administered twice daily it has been as effective as standard therapeutic agents. The side effect profile of acebutolol appears to be comparable to that of other cardioselective beta-blockers. Its relative cardio-selectivity, partial agonist and membrane stabilising activity, hydrophilicity, and considerable extrarenal excretion may offer advantages over some beta-blocking drugs in specific patients. Choosing a beta-blocking agent, however, should be made with a knowledge of pharmacodynamic and pharmacokinetic properties of the various agents and careful consideration of how such properties may be of benefit to an individual patient.
Topics: Acebutolol; Angina Pectoris; Animals; Anti-Arrhythmia Agents; Arrhythmias, Cardiac; Blood Vessels; Bronchi; Central Nervous System; Diabetes Mellitus; Dogs; Female; Heart; Humans; Hypertension; Infant, Newborn; Kidney Diseases; Kinetics; Metabolism; Pregnancy; Rats; Respiration
PubMed: 3891306
DOI: 10.2165/00003495-198529060-00003 -
British Journal of Clinical Pharmacology Oct 1979
Topics: Acebutolol; Acetylation; Adult; Biotransformation; Female; Humans; Hydrogen-Ion Concentration; Male; Saliva
PubMed: 41552
DOI: 10.1111/j.1365-2125.1979.tb04724.x -
American Heart Journal Apr 1991
Comparative Study Review
Topics: Acebutolol; Arrhythmias, Cardiac; Chronic Disease; Clinical Trials as Topic; Humans
PubMed: 2008843
DOI: 10.1016/0002-8703(91)90681-7 -
Drugs 1988Epidemiological and recent interventional studies have emphasised the relationship between plasma lipid parameters and the incidence of coronary heart disease.... (Comparative Study)
Comparative Study Review
Epidemiological and recent interventional studies have emphasised the relationship between plasma lipid parameters and the incidence of coronary heart disease. beta-Blockers, particularly those without intrinsic sympathomimetic activity (ISA), are generally reported to increase triglyceride levels and decrease high density lipoprotein (HDL)-cholesterol levels, both changes theoretically increasing the risk of coronary heart disease. A review of all published trials concerning the effects of acebutolol (a cardioselective beta-blocker with mild ISA) on the plasma lipid profile was carried out, with a particular emphasis on studies reporting a comparison with other beta-blockers. The results indicate that, on average, acebutolol does not have any adverse effects on plasma lipids and may even reduce total and low density lipoprotein (LDL)-cholesterol by 7 and 5%, respectively. In contrast, the other beta-blockers compared under the same conditions (propranolol, pindolol and penbutolol) tended to increase triglyceride levels (+19% when compared with acebutolol) and decrease HDL-cholesterol (-7% when compared with acebutolol) to an extent that was consistent with previous reports in the literature. In interpreting these differences in lipid parameters in the light of epidemiological and interventional study data, the use of acebutolol as opposed to the other beta-blockers could theoretically lead to a relative reduction in coronary risk of 20% or more.
Topics: Acebutolol; Cholesterol; Humans; Lipoproteins; Penbutolol; Pindolol; Propranolol; Triglycerides
PubMed: 3063505
DOI: 10.2165/00003495-198800362-00008 -
The Medical Letter on Drugs and... Jul 1985
Clinical Trial
Topics: Acebutolol; Arrhythmias, Cardiac; Clinical Trials as Topic; Heart Ventricles; Humans; Hypertension; Kinetics
PubMed: 3892259
DOI: No ID Found -
British Medical Journal (Clinical... Jan 1983
Topics: Acebutolol; Aged; Alveolitis, Extrinsic Allergic; Drug Hypersensitivity; Humans; Male
PubMed: 6402066
DOI: 10.1136/bmj.286.6361.266-a -
British Journal of Clinical Pharmacology Sep 1983Acebutolol was administered orally in a single dose of 200 mg to 17 individuals whose renal function varied markedly. The plasma half-life and elimination rate constant...
Acebutolol was administered orally in a single dose of 200 mg to 17 individuals whose renal function varied markedly. The plasma half-life and elimination rate constant for acebutolol showed a four-fold variation but these did not correlate with the degree of renal impairment. However, there was a good correlation between the renal clearance of creatinine and that of acebutolol (P less than 0.001). The half-life and elimination rate of the acetyl metabolite, diacetolol, were subject to 10-fold inter-individual variability which correlated significantly with the creatinine clearance and serum creatinine concentration. The AUC for the acetyl metabolite showed a 40-fold individual variation which also correlated with renal function. It is concluded that renal elimination is the principal route of excretion for diacetolol but not the parent compound, acebutolol.
Topics: Acebutolol; Acetylation; Adult; Biotransformation; Creatinine; Female; Humans; Kidney Failure, Chronic; Kinetics; Male; Middle Aged
PubMed: 6626416
DOI: 10.1111/j.1365-2125.1983.tb02158.x -
Clinical Pharmacology and Therapeutics Feb 1979The effect of intravenous acebutolol on supraventricular arrhythmias was evaluated in 20 patients, 5 with chronic obstructive pulmonary disease. A rapid ventricular rate... (Clinical Trial)
Clinical Trial Comparative Study
The effect of intravenous acebutolol on supraventricular arrhythmias was evaluated in 20 patients, 5 with chronic obstructive pulmonary disease. A rapid ventricular rate in atrial fibrillation was slowed greater than 15% in all of 10 patients by acebutolol and in none of 5 patients by saline. A rapid ventricular rate in atrial flutter was slowed greater than 15% in all of 6 patients by acebutolol and in none of 3 patients by saline. Frequent premature atrial beats were abolished or reduced by greater than 75% in each of 2 patients by acebutolol and not in a patient by saline. Acebutolol converted multifocal atrial tachycardia to sinus rhythm in a patient. Digitalis-induced nonparoxysmal atrioventricular junctional tachycardia was not affected by saline but was abolished by acebutolol in a patient. Acebutolol was well tolerated in each of 5 patients with chronic obstructive pulmonary disease. Acebutolol is useful in the treatment of supraventricular arrhythmias.
Topics: Acebutolol; Adult; Aged; Arrhythmias, Cardiac; Clinical Trials as Topic; Double-Blind Method; Heart Rate; Humans; Injections, Intravenous; Male; Middle Aged
PubMed: 365429
DOI: 10.1002/cpt1979252149