II. Indications
III. Mechanism
- See Beta Adrenergic ReceptorAntagonist
- Acebutolol is unique in that it also has weak intrinsic Sympathomimetic activity (partial beta Agonist)
- Similar intrinsic Sympathomimetic activity (ISA) is seen with Pindolol
- Other selective Beta Blockers without ISA activity are preferred in Coronary Artery Disease
- Like other Selective Beta Antagonists, it primarily inhibits B1 activity by blocking B1 Receptors
- Reduces Myocardial Contractility, Blood Pressure, myocardial oxygen demand
- Also Antiarrhythmic and slows ventricular response in Atrial Fibrillation
- Contrast with non-selective Beta Blockers (e.g. Propranolol)
- Non-selective Beta Blockers also act at B2 Receptors (bronchoconstriction) and B3 Receptors (block lipolysis)
IV. Adverse Effects
- See Beta Blocker
V. Drug Interactions
- See Beta Blocker
VI. Dosing
- Start: 400 mg orally daily or divided 200 mg orally twice daily
- Better efficacy when divided twice daily
- Target: 400 to 800 mg/day
- Maximum: 1200 mg/day
VII. Safety
- Pregnancy Category B
- Avoid in Lactation
VIII. Metabolism
- Not lipophilic
-
Bioavailability 40%
- High first pass hepatic metabolism to a renally excreted metabolite
IX. Resources
X. References
- (2019) Presc Lett, Resource #350503, Comparison of Oral Beta Blockers
- (2020) Med Lett Drugs Ther 62(1598): 73-80
- Olson (2020) Clinical Pharmacology, Medmaster Miami, p. 66-7
- Hamilton (2020) Tarascon Pocket Pharmacopoeia
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Related Studies
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 |