Description

Simple

A medication used to control high blood pressure and irregular heartbeats.

Clinical

A selective β1-receptor antagonist used for the management of hypertension and ventricular premature beats in adults.

Overview

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.

Pharmacology

Indication

For the management of hypertension and ventricular premature beats in adults.

Pharmacodynamic

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 antag... Read more

Mechanism of action

Acebutolol is a selective β1-receptor antagonist. Activation of β1-receptors by epinephrine increases the heart rate and the blood pressure, and the heart consumes more oxygen. Acebutolol blocks these receptors, lowering the heart rate and blood pressure. This drug then has the reverse eff... Read more

Absorption

Well absorbed from the Gl tract with an absolute bioavailability of approximately 40% for the parent compound. In

Protein binding

26%

Volume of distribution

Information currently not available.

Clearance

Information currently not available.

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.

Route of 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.

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.

Adverse Effects

Contraindications

  • Regions: US
  • Patient Conditions:
      • Name: Overt cardiac failure
      • Drugbank Id: DBCOND0107647
  • Regions: US
  • Patient Conditions:
      • Name: Cardiogenic Shock
      • Drugbank Id: DBCOND0030788
  • Regions: US
  • Patient Conditions:
      • Name: Persistently severe bradycardia
      • Drugbank Id: DBCOND0108261
  • Regions: US
  • Patient Conditions:
      • Name: Second- and third-degree heart block
      • Drugbank Id: DBCOND0108262

Food Interactions

  • Take with or without food. Food decreases absorption rate and maximum concentration, but not to a clinically significant extent.

Interactions

Type in a drug name to check for interaction with Acebutolol
Type a drug name in the box above to get started
  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
1-(2-Phenylethyl)-4-phenyl-4-acetoxypiperidine
The metabolism of Acebutolol can be decreased when combined with 1-(2-Phenylethyl)-4-phenyl-4-acetoxypiperidine.
1-benzylimidazole
1-benzylimidazole may decrease the antihypertensive activities of Acebutolol.
1,10-Phenanthroline
1,10-Phenanthroline may increase the bradycardic activities of Acebutolol.
2,4-thiazolidinedione
The therapeutic efficacy of 2,4-thiazolidinedione can be increased when used in combination with Acebutolol.
2,5-Dimethoxy-4-ethylamphetamine
The therapeutic efficacy of Acebutolol can be decreased when used in combination with 2,5-Dimethoxy-4-ethylamphetamine.
2,5-Dimethoxy-4-ethylthioamphetamine
The therapeutic efficacy of Acebutolol can be decreased when used in combination with 2,5-Dimethoxy-4-ethylthioamphetamine.
25-desacetylrifapentine
The metabolism of Acebutolol can be increased when combined with 25-desacetylrifapentine.
3-isobutyl-1-methyl-7H-xanthine
The risk or severity of adverse effects can be increased when Acebutolol is combined with 3-isobutyl-1-methyl-7H-xanthine.
3,5-diiodothyropropionic acid
The risk or severity of adverse effects can be increased when Acebutolol is combined with 3,5-diiodothyropropionic acid.
3,5-Diiodotyrosine
The risk or severity of adverse effects can be increased when Acebutolol is combined with 3,5-Diiodotyrosine.
4-Bromo-2,5-dimethoxyamphetamine
The therapeutic efficacy of Acebutolol can be decreased when used in combination with 4-Bromo-2,5-dimethoxyamphetamine.
4-Bromo-2,5-dimethoxyphenethylamine
The therapeutic efficacy of 4-Bromo-2,5-dimethoxyphenethylamine can be decreased when used in combination with Acebutolol.
4-Methoxyamphetamine
The therapeutic efficacy of 4-Methoxyamphetamine can be decreased when used in combination with Acebutolol.
5-methoxy-N,N-dimethyltryptamine
The metabolism of Acebutolol can be decreased when combined with 5-methoxy-N,N-dimethyltryptamine.
6-O-benzylguanine
The risk or severity of adverse effects can be increased when Acebutolol is combined with 6-O-benzylguanine.
7-Deazaguanine
The risk or severity of adverse effects can be increased when Acebutolol is combined with 7-Deazaguanine.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline may increase the hypotensive activities of Acebutolol.
7,9-Dimethylguanine
The risk or severity of adverse effects can be increased when Acebutolol is combined with 7,9-Dimethylguanine.
8-azaguanine
The risk or severity of adverse effects can be increased when Acebutolol is combined with 8-azaguanine.
8-chlorotheophylline
The risk or severity of adverse effects can be increased when Acebutolol is combined with 8-chlorotheophylline.