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
Images: Related links to external sites (from Bing)
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 |