Acebutolol

Abstract

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.

Discovery and Mechanistic Understanding of a Lipase from Rhizorhabdus dicambivorans for Efficient Ester Aminolysis in Aromatic Amines

“…The amide formed in the reaction between 2 h and 1 a can be used as an intermediate of an endogenous, reactive oxygen species (ROS)‐activated histone deacetylase inhibitor prodrug for cancer chemotherapy [23] . The amide synthesized in the reaction between 1 a and 2 d is less efficient (~40 % conversion) but also leads to the formation of a valuable intermediate for the synthesis of acebutolol, a drug for the treatment of angina pectoris [24] . This disparity in activity could potentially be attributed to the unfavorable binding conformation of small substrates within the spacious substrate‐binding pocket.…”

“…[23] The amide synthesized in the reaction between 1 a and 2 d is less efficient (~40 % conversion) but also leads to the formation of a valuable intermediate for the synthesis of acebutolol, a drug for the treatment of angina pectoris. [24] This disparity in activity could potentially be attributed to the unfavorable binding conformation of small substrates within the spacious substrate-binding pocket. In a related study, the binding pocket of an aminotransferase that catalyzes the synthesis of valienamine (an intermediate in the synthesis of the anti-diabetic drug acarbose and the antibiotic validamycin) was modified to optimize the binding interactions of smaller substrates in an active site that accommodates larger substrates.…”

Evaluation of antinociceptive effect and pharmacological mechanisms of thiocyanoacetamide in rats

“…Acebutolol is a “cardioselective” β1‐receptor antagonist used for the management of hypertension and ventricular premature beats in adults 42 . It has fewer antagonistic effects on peripheral vascular ß2‐receptors at rest and after epinephrine stimulation than nonselective beta‐antagonists.…”

Beta-Adrenergic Blockers’ Supportive and Adverse Role in Hypertension: A Review of Three Generations

“…Once-daily acebutolol as monotherapy is claimed to give effective control in a vast majority of people with mild to moderate essential hypertension, and when administered in conjunction with diuretics results in a further reduction in BP. Acebutolol, on the other hand, has documented side effects include dizziness, headache, fatigue, and gastrointestinal distress, which are also common with all β blockers 35 .…”