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

Effect Regions Age Groups Incidences Evidence Type
Fatigue US
  • Kind: experimental
    • Percent: 11%
  • Kind: placebo
    • Percent: 4%
  • Kind: comparator
    • Percent: 10%
  • Kind: comparator
    • Percent: 17%
  • Clinical Trial
    Fatigue US
  • Kind: experimental
    • Percent: 11%
  • Kind: placebo
    • Percent: 4%
  • Kind: comparator
    • Percent: 10%
  • Kind: comparator
    • Percent: 17%
  • Clinical Trial
    Fatigue US
  • Kind: experimental
    • Percent: 11%
  • Kind: placebo
    • Percent: 4%
  • Kind: comparator
    • Percent: 10%
  • Kind: comparator
    • Percent: 17%
  • Clinical Trial
    Headache US
  • Kind: experimental
    • Percent: 6%
  • Kind: placebo
    • Percent: 4%
  • Kind: comparator
    • Percent: 9%
  • Kind: comparator
    • Percent: 13%
  • Clinical Trial
    Headache US
  • Kind: experimental
    • Percent: 6%
  • Kind: placebo
    • Percent: 4%
  • Kind: comparator
    • Percent: 9%
  • Kind: comparator
    • Percent: 13%
  • Clinical Trial
    Headache US
  • Kind: experimental
    • Percent: 6%
  • Kind: placebo
    • Percent: 4%
  • Kind: comparator
    • Percent: 13%
  • Kind: comparator
    • Percent: 9%
  • Clinical Trial
    Dizziness US
  • Kind: experimental
    • Percent: 6%
  • Kind: placebo
    • Percent: 2%
  • Kind: comparator
    • Percent: 12%
  • Kind: comparator
    • Percent: 7%
  • Clinical Trial
    Dizziness US
  • Kind: experimental
    • Percent: 6%
  • Kind: placebo
    • Percent: 2%
  • Kind: comparator
    • Percent: 7%
  • Kind: comparator
    • Percent: 12%
  • Clinical Trial
    Dizziness US
  • Kind: experimental
    • Percent: 6%
  • Kind: placebo
    • Percent: 2%
  • Kind: comparator
    • Percent: 7%
  • Kind: comparator
    • Percent: 12%
  • Clinical Trial
    Increased micturition US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: <1%
  • Kind: comparator
    • Percent: 1%
  • Kind: comparator
    • Percent: 9%
  • Clinical Trial
    Increased micturition US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: <1%
  • Kind: comparator
    • Percent: 9%
  • Kind: comparator
    • Percent: 1%
  • Clinical Trial
    Increased micturition US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: <1%
  • Kind: comparator
    • Percent: 9%
  • Kind: comparator
    • Percent: 1%
  • Clinical Trial
    Constipation US
  • Kind: experimental
    • Percent: 4%
  • Kind: placebo
    • Percent: 0%
  • Kind: comparator
    • Percent: 2%
  • Kind: comparator
    • Percent: 7%
  • Clinical Trial
    Constipation US
  • Kind: experimental
    • Percent: 4%
  • Kind: placebo
    • Percent: 0%
  • Kind: comparator
    • Percent: 7%
  • Kind: comparator
    • Percent: 2%
  • Clinical Trial
    Constipation US
  • Kind: experimental
    • Percent: 4%
  • Kind: placebo
    • Percent: 0%
  • Kind: comparator
    • Percent: 7%
  • Kind: comparator
    • Percent: 2%
  • Clinical Trial
    Flatulence US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 1%
  • Kind: comparator
    • Percent: 7%
  • Kind: comparator
    • Percent: 4%
  • Clinical Trial
    Flatulence US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 1%
  • Kind: comparator
    • Percent: 4%
  • Kind: comparator
    • Percent: 7%
  • Clinical Trial
    Flatulence US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 1%
  • Kind: comparator
    • Percent: 4%
  • Kind: comparator
    • Percent: 7%
  • Clinical Trial
    Nausea US
  • Kind: experimental
    • Percent: 4%
  • Kind: placebo
    • Percent: 0%
  • Kind: comparator
    • Percent: 6%
  • Kind: comparator
    • Percent: 3%
  • Clinical Trial
    Nausea US
  • Kind: experimental
    • Percent: 4%
  • Kind: placebo
    • Percent: 0%
  • Kind: comparator
    • Percent: 3%
  • Kind: comparator
    • Percent: 6%
  • Clinical Trial
    Dyspnea US
  • Kind: experimental
    • Percent: 4%
  • Kind: placebo
    • Percent: 2%
  • Kind: comparator
    • Percent: 4%
  • Kind: comparator
    • Percent: 6%
  • Clinical Trial
    Dyspnea US
  • Kind: experimental
    • Percent: 4%
  • Kind: placebo
    • Percent: 2%
  • Kind: comparator
    • Percent: 6%
  • Kind: comparator
    • Percent: 4%
  • Clinical Trial
    Dyspnea US
  • Kind: experimental
    • Percent: 4%
  • Kind: placebo
    • Percent: 2%
  • Kind: comparator
    • Percent: 6%
  • Kind: comparator
    • Percent: 4%
  • Clinical Trial
    Nausea US
  • Kind: experimental
    • Percent: 4%
  • Kind: placebo
    • Percent: 0%
  • Kind: comparator
    • Percent: 3%
  • Kind: comparator
    • Percent: 6%
  • Clinical Trial
    Dyspepsia US
  • Kind: experimental
    • Percent: 4%
  • Kind: placebo
    • Percent: 1%
  • Kind: comparator
    • Percent: 3%
  • Kind: comparator
    • Percent: 6%
  • Clinical Trial
    Dyspepsia US
  • Kind: experimental
    • Percent: 4%
  • Kind: placebo
    • Percent: 1%
  • Kind: comparator
    • Percent: 3%
  • Kind: comparator
    • Percent: 6%
  • Clinical Trial
    Dyspepsia US
  • Kind: experimental
    • Percent: 4%
  • Kind: placebo
    • Percent: 1%
  • Kind: comparator
    • Percent: 3%
  • Kind: comparator
    • Percent: 6%
  • Clinical Trial
    Insomnia US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 1%
  • Kind: comparator
    • Percent: 6%
  • Kind: comparator
    • Percent: 5%
  • Clinical Trial
    Insomnia US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 1%
  • Kind: comparator
    • Percent: 5%
  • Kind: comparator
    • Percent: 6%
  • Clinical Trial
    Insomnia US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 1%
  • Kind: comparator
    • Percent: 5%
  • Kind: comparator
    • Percent: 6%
  • Clinical Trial
    Diarrhea US
  • Kind: experimental
    • Percent: 4%
  • Kind: placebo
    • Percent: 1%
  • Kind: comparator
    • Percent: 5%
  • Kind: comparator
    • Percent: 5%
  • Clinical Trial
    Diarrhea US
  • Kind: experimental
    • Percent: 4%
  • Kind: placebo
    • Percent: 1%
  • Kind: comparator
    • Percent: 5%
  • Kind: comparator
    • Percent: 5%
  • Clinical Trial
    Diarrhea US
  • Kind: experimental
    • Percent: 4%
  • Kind: placebo
    • Percent: 1%
  • Kind: comparator
    • Percent: 5%
  • Kind: comparator
    • Percent: 5%
  • Clinical Trial
    Chest Pain US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 1%
  • Kind: comparator
    • Percent: 4%
  • Kind: comparator
    • Percent: 4%
  • Clinical Trial
    Chest Pain US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 1%
  • Kind: comparator
    • Percent: 4%
  • Kind: comparator
    • Percent: 4%
  • Clinical Trial
    Edema US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 1%
  • Kind: comparator
    • Percent: 2%
  • Kind: comparator
    • Percent: 4%
  • Clinical Trial
    Chest Pain US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 1%
  • Kind: comparator
    • Percent: 4%
  • Kind: comparator
    • Percent: 4%
  • Clinical Trial
    Rhinitis US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: <1%
  • Kind: comparator
    • Percent: 4%
  • Kind: comparator
    • Percent: 1%
  • Clinical Trial
    Myalgia US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 0%
  • Kind: comparator
    • Percent: 4%
  • Kind: comparator
    • Percent: 1%
  • Clinical Trial
    Myalgia US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 0%
  • Kind: comparator
    • Percent: 1%
  • Kind: comparator
    • Percent: 4%
  • Clinical Trial
    Rhinitis US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: <1%
  • Kind: comparator
    • Percent: 4%
  • Kind: comparator
    • Percent: 1%
  • Clinical Trial
    Rhinitis US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: <1%
  • Kind: comparator
    • Percent: 1%
  • Kind: comparator
    • Percent: 4%
  • Clinical Trial
    Myalgia US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 0%
  • Kind: comparator
    • Percent: 4%
  • Kind: comparator
    • Percent: 1%
  • Clinical Trial
    Rash US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 1%
  • Kind: comparator
    • Percent: 2%
  • Kind: comparator
    • Percent: 4%
  • Clinical Trial
    Rash US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 1%
  • Kind: comparator
    • Percent: 2%
  • Kind: comparator
    • Percent: 4%
  • Clinical Trial
    Rash US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 1%
  • Kind: comparator
    • Percent: 4%
  • Kind: comparator
    • Percent: 2%
  • Clinical Trial
    Edema US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 1%
  • Kind: comparator
    • Percent: 4%
  • Kind: comparator
    • Percent: 2%
  • Clinical Trial
    Edema US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 1%
  • Kind: comparator
    • Percent: 2%
  • Kind: comparator
    • Percent: 4%
  • Clinical Trial
    Abnormal vision US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 0%
  • Kind: comparator
    • Percent: 3%
  • Kind: comparator
    • Percent: 2%
  • Clinical Trial
    Abnormal vision US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 0%
  • Kind: comparator
    • Percent: 3%
  • Kind: comparator
    • Percent: 2%
  • Clinical Trial

    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.