Acebutolol

— THERAPEUTIC CATEGORIES —
  • CHF and arrhythmias
  • Hypertension
PAGE CONTENTS
  • Jump to Section
  • Generic Name & Formulations
  • Indications
  • Dosage and Administration
  • Contraindications
  • Boxed Warnings
  • Warnings/Precautions
  • Pharmacokinetics
  • Interactions
  • Adverse Reactions
  • Clinical Trials
  • Note
  • Patient Counseling

    • Acebutolol Generic Name & Formulations

    Legal Class

    Rx

    General Description

    Acebutolol (as HCl) 200mg, 400mg; caps.

    Pharmacological Class

    Cardioselective beta-blocker.

    How Supplied

    Contact supplier

    Manufacturer

    Various generic manufacturers

    Acebutolol Indications

    Indications

    Ventricular arrhythmias.

    Acebutolol Dosage and Administration

    Adult

    Initially 200mg twice a day. Usual range: 600mg–1.2g daily.

    Children

    Not established.

    Elderly

    Max 800mg/day.

    Acebutolol Contraindications

    Contraindications

    Severe bradycardia. 2nd- or 3rd-degree AV block. Overt heart failure. Cardiogenic shock.

    Acebutolol Boxed Warnings

    Not Applicable

    Acebutolol Warnings/Precautions

    Warnings/Precautions

    Bronchospastic disease. Ischemic heart disease or failure. Renal or hepatic dysfunction. Diabetes. Hyperthyroidism. Vascular insufficiency. Surgery. Avoid abrupt cessation. Elderly. Pregnancy (Cat.B). Nursing mothers: not recommended.

    Warnings/Precautions

    Cardiac Failure

    • Use acebutolol with caution in patients with a history of heart failure who are controlled with digitalis and/or diuretics.

    • Withdraw acebutolol if cardiac failure persists.

    In Patients Without a History of Cardiac Failure

    • In patients with aortic or mitral valve disease or compromised left ventricular function, continued depression of the myocardium with β-blocking agents over a period of time may lead to cardiac failure.

    • At first signs of failure, patients should be digitalized and/or be given a diuretic and the response observed closely. Withdraw acebutolol therapy if cardiac failure continues despite adequate digitalization and/or diuretic. 

    Exacerbation of Ischemic Heart Disease Following Abrupt Withdrawal

    • Advise patients with coronary artery disease to avoid interrupting therapy without a physician’s advice.

    • Even patients without overt ischemic heart disease should also be carefully observed when acebutolol is discontinued, and should be advised to limit physical activity to a minimum during its gradual withdrawal over a period of about 2 weeks.

    • If angina pectoris occurs, restart antianginal therapy immediately in full doses and hospitalize the patient until his condition stabilizes.

    Peripheral Vascular Disease

    • Exercise caution in patients with peripheral or mesenteric vascular disease, and monitor closely for evidence of progression of arterial obstruction.

    Bronchospastic Disease

    • Do not administer a beta-blocker to patients with bronchospastic disease.

    • However, low doses of acebutolol may be used with caution in these patients who do not respond to, or who cannot tolerate, alternative treatment. Use the lowest possible dose of acebutolol initially, preferably in divided doses to avoid the higher plasma levels associated with the longer dose-interval.

    WARNINGS, Major Surgery

    • Chronically administered beta-blocking therapy should not be routinely withdrawn prior to major surgery.

    Diabetes and Hypoglycemia

    • Warn diabetic patients of the possibility of masked hypoglycemia.

    Thyrotoxicosis

    • Beta-adrenergic blockade may mask clinical signs (tachycardia) of hyperthyroidism.

    • May precipitate a thyroid storm if there is an abrupt withdrawal of beta-blockade.

    • Monitor closely in patients suspected of developing thyrotoxicosis from whom acebutolol therapy who are to be withdrawn.

    Impaired Renal of Hepatic Function

    • Reduce the daily dose of acebutolol by 50% if the CrCl <50mL/min. 

    • Reduce the daily dose of acebutolol by 75% if the CrCl  <25mL/min.

    • Use caution in patients with impaired hepatic function.

    • Elderly patients may require lower maintenance doses.

    Pregnancy Considerations

    Teratogenic Effects

    • Pregnancy Category B: Use acebutolol during pregnancy only if the potential benefit justifies the risk to the fetus.

     

    Geriatric Considerations

    May be appropriate to start elderly patients at the low end of the dosing range.

    Other Considerations for Specific Populations

    Labor and Delivery

    • The effect of acebutolol on labor and delivery in pregnancy women is unknown.

     

    Acebutolol Pharmacokinetics

    Absorption

    Acebutolol is well absorbed from the GI tract. It is subject to extensive first-pass hepatic biotransformation, with an absolute bioavailability of approximately 40% for the parent compound.

    Distribution

    Acebutolol has a low binding affinity for plasma proteins (about 26%). Acebutolol and its metabolite, diacetolol, are relatively hydrophilic and, therefore, only minimal quantities have been detected in the cerebrospinal fluid (CSF).

    Metabolism

    The major metabolite, an N-acetyl derivative (diacetolol), is pharmacologically active. This metabolite is equipotent to acebutolol and in cats is more cardioselective than acebutolol; therefore, this first-pass phenomenon does not attenuate the therapeutic effect of acebutolol. 

    Elimination

    The plasma elimination half-life of acebutolol is approximately 3 to 4 hours, while that of its metabolite, diacetolol, is 8 to 13 hours. Elimination via renal excretion is approximately 30% to 40% and by nonrenal mechanisms 50% to 60%, which includes excretion into the bile and direct passage through the intestinal wall.

    Acebutolol Interactions

    Interactions

    May potentiate hypotension with prazosin, reserpine, other catecholamine-depleting drugs. Antagonized by NSAIDs. May increase cardiac effects of verapamil, digitalis. Avoid α-adrenergic agonists. May block epinephrine.

    Acebutolol Adverse Reactions

    Adverse Reactions

    Fatigue, dizziness, headache, GI upset, dyspnea, dysuria, insomnia, rash, myalgia, rhinitis, abnormal vision, hypotension, bradycardia, heart failure or block, bronchospasm, elevated ANA titers.

    Acebutolol Clinical Trials

    See Literature

    Acebutolol Note

    Notes

    Formerly known under the brand name Sectral.

    Acebutolol Patient Counseling

    Patient Counseling

    • Advise patients with coronary artery disease to avoid interrupting or discontinuing therapy without a physician’s advice.

    • Cardiac failure occurs rarely but patients should be advised to consult a physician if signs or symptoms suggestive of impending CHF or unexplained respiratory symptoms occur.

    • Advise patients that possible severe hypertensive reactions may occur with concomitant use with alpha-adrenergic stimulants (eg, nasal decongestants commonly used in OTC cold preparations and nasal drops).

    Acebutolol Generic Name & Formulations

    Legal Class

    Rx

    General Description

    Acebutolol (as HCl) 200mg, 400mg; caps.

    Pharmacological Class

    Cardioselective beta-blocker.

    How Supplied

    Contact supplier

    Manufacturer

    Various generic manufacturers

    Acebutolol Indications

    Indications

    Hypertension.

    Acebutolol Dosage and Administration

    Adult

    Initially 400mg daily in 1–2 divided doses. Usual range: 200–800mg daily; max 1.2g/day in 2 divided doses.

    Children

    Not established.

    Elderly

    Max 800mg/day.

    Acebutolol Contraindications

    Contraindications

    Severe bradycardia. 2nd- or 3rd-degree AV block. Overt heart failure. Cardiogenic shock.

    Acebutolol Boxed Warnings

    Not Applicable

    Acebutolol Warnings/Precautions

    Warnings/Precautions

    Bronchospastic disease. Ischemic heart disease or failure. Renal or hepatic dysfunction. Diabetes. Hyperthyroidism. Vascular insufficiency. Surgery. Avoid abrupt cessation. Elderly. Pregnancy (Cat.B). Nursing mothers: not recommended.

    Warnings/Precautions

    Cardiac Failure

    • Use acebutolol with caution in patients with a history of heart failure who are controlled with digitalis and/or diuretics.

    • Withdraw acebutolol if cardiac failure persists.

    In Patients Without a History of Cardiac Failure

    • In patients with aortic or mitral valve disease or compromised left ventricular function, continued depression of the myocardium with β-blocking agents over a period of time may lead to cardiac failure.

    • At first signs of failure, patients should be digitalized and/or be given a diuretic and the response observed closely. Withdraw acebutolol therapy if cardiac failure continues despite adequate digitalization and/or diuretic. 

    Exacerbation of Ischemic Heart Disease Following Abrupt Withdrawal

    • Advise patients with coronary artery disease to avoid interrupting therapy without a physician’s advice.

    • Even patients without overt ischemic heart disease should also be carefully observed when acebutolol is discontinued, and should be advised to limit physical activity to a minimum during its gradual withdrawal over a period of about 2 weeks.

    • If angina pectoris occurs, restart antianginal therapy immediately in full doses and hospitalize the patient until his condition stabilizes.

    Peripheral Vascular Disease

    • Exercise caution in patients with peripheral or mesenteric vascular disease, and monitor closely for evidence of progression of arterial obstruction.

    Bronchospastic Disease

    • Do not administer a beta-blocker to patients with bronchospastic disease.

    • However, low doses of acebutolol may be used with caution in these patients who do not respond to, or who cannot tolerate, alternative treatment. Use the lowest possible dose of acebutolol initially, preferably in divided doses to avoid the higher plasma levels associated with the longer dose-interval.

    WARNINGS, Major Surgery

    • Chronically administered beta-blocking therapy should not be routinely withdrawn prior to major surgery.

    Diabetes and Hypoglycemia

    • Warn diabetic patients of the possibility of masked hypoglycemia.

    Thyrotoxicosis

    • Beta-adrenergic blockade may mask clinical signs (tachycardia) of hyperthyroidism.

    • May precipitate a thyroid storm if there is an abrupt withdrawal of beta-blockade.

    • Monitor closely in patients suspected of developing thyrotoxicosis from whom acebutolol therapy who are to be withdrawn.

    Impaired Renal of Hepatic Function

    • Reduce the daily dose of acebutolol by 50% if the CrCl <50mL/min. 

    • Reduce the daily dose of acebutolol by 75% if the CrCl  <25mL/min.

    • Use caution in patients with impaired hepatic function.

    • Elderly patients may require lower maintenance doses.

    Pregnancy Considerations

    Teratogenic Effects

    • Pregnancy Category B: Use acebutolol during pregnancy only if the potential benefit justifies the risk to the fetus.

     

    Geriatric Considerations

    May be appropriate to start elderly patients at the low end of the dosing range.

    Other Considerations for Specific Populations

    Labor and Delivery

    • The effect of acebutolol on labor and delivery in pregnancy women is unknown.

     

    Acebutolol Pharmacokinetics

    Absorption

    Acebutolol is well absorbed from the GI tract. It is subject to extensive first-pass hepatic biotransformation, with an absolute bioavailability of approximately 40% for the parent compound.

    Distribution

    Acebutolol has a low binding affinity for plasma proteins (about 26%). Acebutolol and its metabolite, diacetolol, are relatively hydrophilic and, therefore, only minimal quantities have been detected in the cerebrospinal fluid (CSF).

    Metabolism

    The major metabolite, an N-acetyl derivative (diacetolol), is pharmacologically active. This metabolite is equipotent to acebutolol and in cats is more cardioselective than acebutolol; therefore, this first-pass phenomenon does not attenuate the therapeutic effect of acebutolol. 

    Elimination

    The plasma elimination half-life of acebutolol is approximately 3 to 4 hours, while that of its metabolite, diacetolol, is 8 to 13 hours. Elimination via renal excretion is approximately 30% to 40% and by nonrenal mechanisms 50% to 60%, which includes excretion into the bile and direct passage through the intestinal wall.

    Acebutolol Interactions

    Interactions

    May potentiate hypotension with prazosin, reserpine, other catecholamine-depleting drugs. Antagonized by NSAIDs. May increase cardiac effects of verapamil, digitalis. Avoid α-adrenergic agonists. May block epinephrine.

    Acebutolol Adverse Reactions

    Adverse Reactions

    Fatigue, dizziness, headache, GI upset, dyspnea, dysuria, insomnia, rash, myalgia, rhinitis, abnormal vision, hypotension, bradycardia, heart failure or block, bronchospasm, elevated ANA titers.

    Acebutolol Clinical Trials

    See Literature

    Acebutolol Note

    Notes

    Formerly known under the brand name Sectral.

    Acebutolol Patient Counseling

    Patient Counseling

    • Advise patients with coronary artery disease to avoid interrupting or discontinuing therapy without a physician’s advice.

    • Cardiac failure occurs rarely but patients should be advised to consult a physician if signs or symptoms suggestive of impending CHF or unexplained respiratory symptoms occur.

    • Advise patients that possible severe hypertensive reactions may occur with concomitant use with alpha-adrenergic stimulants (eg, nasal decongestants commonly used in OTC cold preparations and nasal drops).

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