II. Indications

III. Mechanism

  1. See Beta Adrenergic ReceptorAntagonist
  2. Acebutolol is unique in that it also has weak intrinsic Sympathomimetic activity (partial beta Agonist)
    1. Similar intrinsic Sympathomimetic activity (ISA) is seen with Pindolol
    2. Other selective Beta Blockers without ISA activity are preferred in Coronary Artery Disease
  3. Like other Selective Beta Antagonists, it primarily inhibits B1 activity by blocking B1 Receptors
    1. Reduces Myocardial Contractility, Blood Pressure, myocardial oxygen demand
    2. Also Antiarrhythmic and slows ventricular response in Atrial Fibrillation
  4. Contrast with non-selective Beta Blockers (e.g. Propranolol)
    1. Non-selective Beta Blockers also act at B2 Receptors (bronchoconstriction) and B3 Receptors (block lipolysis)

IV. Adverse Effects

V. Drug Interactions

VI. Dosing

  1. Start: 400 mg orally daily or divided 200 mg orally twice daily
    1. Better efficacy when divided twice daily
  2. Target: 400 to 800 mg/day
  3. Maximum: 1200 mg/day

VII. Safety

  1. Pregnancy Category B
  2. Avoid in Lactation

VIII. Metabolism

  1. Not lipophilic
  2. Bioavailability 40%
    1. High first pass hepatic metabolism to a renally excreted metabolite

X. References

  1. (2019) Presc Lett, Resource #350503, Comparison of Oral Beta Blockers
  2. (2020) Med Lett Drugs Ther 62(1598): 73-80
  3. Olson (2020) Clinical Pharmacology, Medmaster Miami, p. 66-7
  4. Hamilton (2020) Tarascon Pocket Pharmacopoeia

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Related Studies

Cost: Medications

acebutolol (on 12/21/2022 at Medicaid.Gov Survey of pharmacy drug pricing)
ACEBUTOLOL 200 MG CAPSULE Generic $0.65 each
ACEBUTOLOL 400 MG CAPSULE Generic $0.89 each

Ontology: Acebutolol (C0000946)

Definition (MSH) A cardioselective beta-1 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.
Definition (NCI) A synthetic butyranilide derivative with hypotensive and antiarrhythmic activity. Acebutolol acts as a cardioselective beta-adrenergic antagonist with little effect on bronchial receptors and has intrinsic sympathomimetic properties. Having stabilizing and quinidine-like effects on cardiac rhythm, Acebutolol is used in ventricular arrhythmias. Other indications include hypertension, alone or in combinations with other agents.
Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH D000070
SnomedCT 391701001, 372815001, 68088000
LNC LP16015-7, MTHU007114
English Acebutolol, Acetobutolol, Butanamide, N-(3-acetyl-4-(2-hydroxy-3-((1-methylethyl)amino)propoxy)phenyl)-, (+-)-, acebutolol, Acebutolol [Chemical/Ingredient], acetobutolol, Acebutolol - chemical, Acebutolol - chemical (substance), ACEBUTOLOL, Acebutolol (product), Acebutolol (substance)
Swedish Acebutolol
Czech acebutolol
Finnish Asebutololi
Italian Acetobutololo, Acebutololo
Russian ATSEBUTOLOL, АЦЕБУТОЛОЛ
Japanese アセブトロール
French Acétobutolol, Acébutolol
Polish Acebutolol
Spanish acebutolol - sustancia química (sustancia), acebutolol - sustancia química, acebutolol (producto), acebutolol, acebutolol (sustancia), Acebutolol
German Acebutolol
Portuguese Acebutolol

Ontology: Sectral (C0036543)

Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH D000070
French Sectral
English sectral, Italfarmaco Brand of Acebutolol Hydrochloride, Monitan, Specia Brand of Acebutolol Hydrochloride, Wyeth Brand of Acebutolol Hydrochloride, Sectral, Rhône Poulenc Rorer Brand of Acebutolol Hydrochloride, Rhône-Poulenc Rorer Brand of Acebutolol Hydrochloride