| Item |
Information |
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Drug Groups
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approved |
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Description
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A cardioselective beta-adrenergic antagonist with little effect on the bronchial receptors. The drug has stabilizing and quinidine-like effects on cardiac rhythm as well as weak inherent sympathomimetic action. [PubChem] |
| Indication |
For the management of hypertension and ventricular premature beats in adults. |
| Pharmacology |
Acebutolol is a cardioselective, beta-adrenoreceptor blocking agent, which possesses mild intrinsic sympathomimetic activity (ISA) in its therapeutically effective dose range. In general, beta-blockers reduce the work the heart has to do and allow it to beat more regularly. Acebutolol has less antagonistic effects on peripheral vascular ß2-receptors at rest and after epinephrine stimulation than nonselective beta-antagonists. Low doses of acebutolol produce less evidence of bronchoconstriction than nonselective agents like propranolol but more than atenolol. |
| Toxicity |
Symptoms of overdose include extreme bradycardia, advanced atrioventricular block, intraventricular conduction defects, hypotension, severe congestive heart failure, seizures, and in susceptible patients, bronchospasm, and hypoglycemia. |
| Affected Organisms |
| • |
Humans and other mammals |
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| Biotransformation |
Subject to extensive first-pass hepatic biotransformation (primarily to diacetolol). |
| Absorption |
Well absorbed from the Gl tract with an absolute bioavailability of approximately 40% for the parent compound. In |
| Half Life |
The plasma elimination half-life is approximately 3 to 4 hours. The half-life of its metabolite, diacetolol, is 8 to 13 hours. |
| Protein Binding |
26% |
| Elimination |
Elimination via renal excretion is approximately 30% to 40% and by non-renal mechanisms 50% to 60%, which includes excretion into the bile and direct passage through the intestinal wall. |
| External Links |
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